ID Source | ID |
---|---|
PubMed CID | 5330286 |
CHEMBL ID | 189963 |
CHEBI ID | 85993 |
SCHEMBL ID | 462630 |
MeSH ID | M0483974 |
Synonym |
---|
6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazin-1-yl)pyridin-2-yl]amino]-8h-pyrido[2,3-d]pyrimidin-7-one |
pd 0332991 |
pyrido-[2,3-d]-pyrimidin-7-one 43 |
8-cyclopentyl-6-acetyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7h,8h-pyrido[2,3-d]pyrimidin-7-one |
bdbm6309 |
6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8h-pyrido[2,3-d]pyrimidin-7-one hydrochloride |
HY-50767 |
pd-0332991 , |
pd-332991 |
6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7(8h)-one |
lqq , |
2EUF , |
CHEMBL189963 |
chebi:85993 , |
palbociclib , |
6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one |
KINOME_3823 |
KINOME_3824 |
A8153 |
pd0332991 , |
571190-30-2 |
pyrido(2,3-d)pyrimidin-7(8h)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(1-piperazinyl)-2-pyridinyl)amino)- |
palbociclib [usan:inn] |
6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-8h-pyrido(2,3-d)pyrimidin-7-one |
g9zf61le7g , |
pd 332991 |
ibrance |
unii-g9zf61le7g |
S4482 |
BCP9001058 |
HMS3265N09 |
HMS3265N10 |
HMS3265M10 |
HMS3265M09 |
571190-30-2 pound not827022-32-2 |
BCPP000125 |
pd 0332991,pd0332991 |
ibrance (tn) |
D10372 |
palbociclib (jan/usan) |
NCGC00263129-01 |
gtpl7380 |
6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[6,5-d]pyrimidin-7-one |
BRD-K51313569-001-01-1 |
AKOS022205241 |
palbociclib [who-dd] |
6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino(pyrido(2,3-d)pyrimidin-7(8h)-one |
palbociclib [orange book] |
6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-8h-pyrido(2,3-d)pyrimidin-7-one |
palbociclib [inn] |
palbociclib [mi] |
palbociclib [usan] |
palbociclib [jan] |
AHJRHEGDXFFMBM-UHFFFAOYSA-N |
6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8h-pyrido[2,3-d]pyrimidin-7-one |
SCHEMBL462630 |
2euf; pd 0332991 |
6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7(8h)-one |
6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8h)-one |
AC-25485 |
FT-0697059 |
6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7h,8h-pyrido[2,3-d]pyrimidin-7-one |
mfcd11840850 |
DB09073 |
EX-A408 |
palbociclib free base |
NCGC00263129-21 |
palbociclib(pd0332991) |
571190-30-2 (free base) |
AS-17016 |
otava-bb 1115529 |
BCP09274 |
Q15269707 |
AMY14886 |
A14427 |
BCP18381 |
[d8]-palbociclib |
6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridyl]amino]pyrido[2,3-d]pyrimidin-7(8h)-one |
SY026143 |
DTXSID40972590 |
HMS3744G13 |
SB40426 |
NCGC00263129-08 |
nsc772256 |
nsc-772256 |
pd 0332991 (palbociclib) |
nsc-758247 |
nsc800815 |
nsc758247 |
nsc-800815 |
NCGC00263129-22 |
6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazin-1-yl)-pyridin-2-yl]amino]-8h-pyrido[2,3-d]pyrimidin-7-one |
BP166224 |
palbociclib- bio-x |
EN300-18531248 |
palbociclibum |
pd 991 |
l01xe33 |
Z2216894329 |
Palbociclib is a cyclin-dependent kinase inhibitor that targets the ATP binding site of CDK4 and CDK6 with similar potency. It is an effective therapy in the real-world older population and is well-tolerated with low levels of clinically significant toxicities.
Palbociclib has clinical activity as a single agent in women with moderately pretreated, oestrogen receptor-positive, HER2-negative advanced breast cancer. The drug has shown satisfactory outcomes when combined with endocrine therapy (ET) in hormone receptor- positive and human epidermal growth factor receptor 2-negative (HR+/HER2-) metastatic Breast Cancer.
Palbociclib did not increase the rate of complete pathological response. efficacy was lower in patients with high versus low cyclin E1.
Palbociclib, a cyclin-dependent kinase 4/6 inhibitor, has demonstrated significantly improved progression-free survival in patients with hormone receptor-positive, HER2-negative, advanced breast cancer.
Cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors are associated with distinct adverse effects (AEs) compared to other targeted therapies. With palbociclib, neutropenia was the most common grade 3 (55%) and 4 (10%) adverse event.
Serum TK1 activity is a promising pharmacodynamic marker of palbociclib in ER+ breast cancer. Its value in predicting response to CDK4/6 inhibitors warrants further investigation.
Excerpt | Reference | Relevance |
---|---|---|
"Initial pharmacokinetic (PK) studies of discovery compounds are conducted in mice to demonstrate exposure prior to conducting efficacy studies." | ( Discovery pharmacokinetic studies in mice using serial microsampling, dried blood spots and microbore LC-MS/MS. Batugo, M; Nguyen, L; Rahavendran, SV; Shen, Z; Shetty, B; Skor, H; Vekich, S, 2012) | 0.38 |
" The objectives of the current study are to (1) develop a physiologically based pharmacokinetic (PBPK) model of palbociclib based on the in silico, in vitro, and in vivo pharmacokinetic data of palbociclib, (2) verify the PBPK model with clinical drug-drug interaction (DDI) results of palbociclib with strong CYP3A inhibitor (itraconazole), inducer (rifampin), and a sensitive CYP3A substrate (midazolam), and (3) predict the DDI risk of palbociclib with moderate/weak CYP3A inhibitors." | ( Physiologically Based Pharmacokinetic Modeling of Palbociclib. Hoffman, J; Loi, CM; Wang, D; Yu, Y, 2017) | 0.92 |
"Serum TK1 activity is a promising pharmacodynamic marker of palbociclib in ER+ breast cancer, and its value in predicting response to CDK4/6 inhibitors warrants further investigation." | ( Serum thymidine kinase 1 activity as a pharmacodynamic marker of cyclin-dependent kinase 4/6 inhibition in patients with early-stage breast cancer receiving neoadjuvant palbociclib. Bagegni, N; Bergqvist, M; Ellis, M; Forero, A; Goetz, MP; Guo, Z; Hoog, J; Karen, J; Liu, N; Luo, J; Ma, CX; Neumüller, M; Northfelt, DW; Sanati, S; Suh, EM; Thomas, S; Vij, K, 2017) | 0.89 |
" In this review, we provide an overview of the available clinical pharmacokinetic and pharmacodynamic characteristics of these novel drugs, summarize the results of food-effect and drug-drug interaction studies, and highlight exposure-response and exposure-toxicity relationships." | ( Clinical Pharmacokinetics and Pharmacodynamics of the Cyclin-Dependent Kinase 4 and 6 Inhibitors Palbociclib, Ribociclib, and Abemaciclib. Beijnen, JH; Groenland, SL; Huitema, ADR; Martínez-Chávez, A; Schinkel, AH; Steeghs, N; van Dongen, MGJ, 2020) | 0.78 |
"Identification of a pharmacodynamic (PD) biomarker, which is predictive of the efficacy outcome, is of ultimate interest in drug development." | ( Pharmacodynamic Modeling of CDK4/6 Inhibition-Related Biomarkers and the Characterization of the Relationship Between Biomarker Response and Progression-Free Survival in Patients With Advanced Breast Cancer. Liu, Y; Sun, W; Wang, D; Yu, Y, 2022) | 0.72 |
Treatment with palbociclib in combination with AI or fulvestrant demonstrated favorable effectiveness in terms of progression-free and survival rates. Rhabdomyolysis was most likely induced by toxic plasma concentrations of Simvastatin.
The oral bioavailability of palbociclib was high (63%) in WT mice and increased only modestly and non-significantly in Abcg2; Abcb1a/b(-/-) mice.
Palbociclib, when administered with letrozole at the recommended therapeutic dosing regimen, did not prolong the QT interval to a clinically relevant extent. Oncologists in real-world practice have prescribed alternative dosing strategies with palbocIClib.
Role | Description |
---|---|
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of cyclin-dependent kinase (EC 2.7.11.22). |
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
pyridopyrimidine | Any organic heterobicyclic compound consisting of a pyridine ring ortho-fused at any position to a pyrimidine ring. |
aminopyridine | Compounds containing a pyridine skeleton substituted by one or more amine groups. |
secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
piperidines | |
aromatic ketone | A ketone in which the carbonyl group is attached to an aromatic ring. |
cyclopentanes | Cyclopentane and its derivatives formed by substitution. |
tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Fumarate hydratase | Homo sapiens (human) | Potency | 33.1734 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
PPM1D protein | Homo sapiens (human) | Potency | 14.7403 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 15.0916 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 14.9153 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
polyprotein | Zika virus | Potency | 33.1734 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 6.8835 | 0.0000 | 5.0182 | 79.2586 | AID686947 |
Interferon beta | Homo sapiens (human) | Potency | 14.7403 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 31.6228 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Bone morphogenetic protein receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.1413 | 3.7000 | AID1424922 |
Membrane-associated progesterone receptor component 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2040 | 0.2040 | 0.2040 | AID1425109 |
Cell division cycle 7-related protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.5110 | 0.5110 | 0.5110 | AID1424936 |
Serine/threonine-protein kinase PLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.5144 | 9.0000 | AID1425121 |
ATP-dependent RNA helicase DDX3X | Homo sapiens (human) | Kd | 30.0000 | 0.4350 | 0.4350 | 0.4350 | AID1424975 |
Pyridoxal kinase | Homo sapiens (human) | Kd | 30.0000 | 0.2860 | 5.0765 | 16.4040 | AID1425106 |
Citron Rho-interacting kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 3.0646 | 48.8760 | AID1424954 |
Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | Kd | 30.0000 | 0.0028 | 1.4744 | 8.7000 | AID1424953 |
Aurora kinase A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.7342 | 9.3000 | AID1424917 |
Cyclin-G-associated kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 0.9086 | 28.6510 | AID1425009 |
Ephrin type-B receptor 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0768 | 9.0000 | AID1424995 |
Peroxisomal acyl-coenzyme A oxidase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.3140 | 2.6020 | AID1424896 |
Receptor-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6212 | 11.4330 | AID1425155 |
Mitotic checkpoint serine/threonine-protein kinase BUB1 | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 1.3910 | 3.5070 | AID1424926 |
Dynamin-like 120 kDa protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 0.3610 | 0.7050 | AID1425097 |
Rho-associated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.7105 | 56.0660 | AID1425158 |
Serine/threonine-protein kinase ULK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.8410 | 23.2730 | AID1425208 |
Serine/threonine-protein kinase/endoribonuclease IRE1 | Homo sapiens (human) | Kd | 30.0000 | 0.0057 | 2.0095 | 12.2010 | AID1424997 |
Ribosomal protein S6 kinase alpha-5 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 1.9737 | 29.9570 | AID1425162 |
U5 small nuclear ribonucleoprotein 200 kDa helicase | Homo sapiens (human) | Kd | 30.0000 | 1.3820 | 1.3820 | 1.3820 | AID1425174 |
Ribosomal protein S6 kinase alpha-4 | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.6396 | 7.2000 | AID1425161 |
Serine/threonine-protein kinase 16 | Homo sapiens (human) | Kd | 9.9690 | 0.0017 | 1.2483 | 9.9690 | AID1425179 |
Cyclin-dependent kinase-like 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.4788 | 7.3000 | AID1424951 |
Serine/threonine-protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 2.9234 | 57.4530 | AID1425177 |
Serine/threonine-protein kinase D3 | Homo sapiens (human) | Kd | 16.2960 | 0.0089 | 2.2738 | 23.3410 | AID1425137 |
Structural maintenance of chromosomes protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.2090 | 0.6575 | 1.1060 | AID1425173 |
Mitogen-activated protein kinase kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 1.5781 | 8.0000 | AID1425050 |
Mitogen-activated protein kinase kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0082 | 2.3645 | 62.7720 | AID1425054 |
Serine/threonine-protein kinase LATS1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 1.8393 | 10.7330 | AID1425033 |
Serine/threonine-protein kinase PAK 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0027 | 2.5694 | 30.3710 | AID1425100 |
Tyrosine-protein kinase ABL1 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0411 | 13.4530 | AID1424890 |
Epidermal growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.3514 | 20.8270 | AID1424983 |
High affinity nerve growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.3484 | 9.2000 | AID1425094 |
Guanine nucleotide-binding protein G(i) subunit alpha-2 | Homo sapiens (human) | Kd | 30.0000 | 0.1840 | 0.1840 | 0.1840 | AID1425011 |
ADP/ATP translocase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.4510 | 0.4510 | 0.4510 | AID1425169 |
Protein kinase C beta type | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 2.7081 | 26.3240 | AID1425130 |
Insulin receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.0823 | 7.9060 | AID1425026 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1174 | 24.2210 | AID1425034 |
Tyrosine-protein kinase Fyn | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.4238 | 8.4000 | AID1425008 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2880 | 1.4952 | 3.0490 | AID1424937 |
Glycogen phosphorylase, liver form | Homo sapiens (human) | Kd | 30.0000 | 2.1210 | 2.1210 | 2.1210 | AID1425146 |
Tyrosine-protein kinase Fes/Fps | Homo sapiens (human) | Kd | 30.0000 | 0.0048 | 1.0986 | 7.4000 | AID1425003 |
Tyrosine-protein kinase Yes | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.3708 | 17.1520 | AID1425212 |
Tyrosine-protein kinase Lyn | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0485 | 5.7000 | AID1425037 |
Proto-oncogene tyrosine-protein kinase receptor Ret | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 0.8642 | 27.5420 | AID1425154 |
Insulin-like growth factor 1 receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.9211 | 19.2170 | AID1425022 |
Signal recognition particle receptor subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 0.0080 | 0.0080 | AID1425176 |
Cytochrome c1, heme protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.2020 | 0.2020 | AID1424969 |
Hepatocyte growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6297 | 8.5000 | AID1425076 |
Tyrosine-protein kinase HCK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0343 | 15.9930 | AID1425017 |
Platelet-derived growth factor receptor beta | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.0050 | 11.1070 | AID1425104 |
Serine/threonine-protein kinase A-Raf | Homo sapiens (human) | Kd | 30.0000 | 0.0470 | 9.6832 | 33.6550 | AID1424915 |
Glycogen phosphorylase, brain form | Homo sapiens (human) | Kd | 30.0000 | 3.5690 | 3.5690 | 3.5690 | AID1425145 |
Breakpoint cluster region protein | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2196 | 17.3640 | AID1424919 |
Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.1393 | 19.3160 | AID1425111 |
Fibroblast growth factor receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5581 | 6.2000 | AID1425004 |
DNA topoisomerase 2-alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0640 | 0.2750 | 0.4860 | AID1425202 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | Kd | 0.5720 | 0.0033 | 1.6050 | 8.6000 | AID1424946 |
ADP/ATP translocase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 0.2505 | 0.4950 | AID1425170 |
Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.5077 | 9.6000 | AID1425175 |
cAMP-dependent protein kinase type II-alpha regulatory subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0520 | 1.7535 | 3.4550 | AID1425128 |
Serine/threonine-protein kinase B-raf | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6258 | 26.0180 | AID1424924 |
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.0569 | 9.5000 | AID1425110 |
Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 6.7556 | 88.9030 | AID1425093 |
Tyrosine-protein kinase Fer | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 1.3604 | 8.8000 | AID1425002 |
Protein kinase C alpha type | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7922 | 21.3520 | AID1425129 |
cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 2.9479 | 23.2450 | AID1425123 |
General transcription and DNA repair factor IIH helicase subunit XPD | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6906 | 12.0220 | AID1424996 |
Casein kinase II subunit alpha' | Homo sapiens (human) | Kd | 0.4880 | 0.0010 | 2.5309 | 28.8720 | AID1424968 |
Ras-related protein Rab-6A | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 0.0330 | 0.0330 | AID1425150 |
Multifunctional protein ADE2 | Homo sapiens (human) | Kd | 30.0000 | 5.4810 | 5.4810 | 5.4810 | AID1425098 |
cAMP-dependent protein kinase catalytic subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 8.5577 | 49.2780 | AID1425125 |
cAMP-dependent protein kinase catalytic subunit beta | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 0.7408 | 4.1000 | AID1425124 |
Ferrochelatase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2430 | 6.4343 | 67.9140 | AID1425001 |
Ribosomal protein S6 kinase beta-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 1.1805 | 4.8000 | AID1425164 |
Tyrosine-protein kinase JAK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 1.2166 | 7.8000 | AID1425030 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.5179 | 10.4870 | AID1424944 |
Beta-adrenergic receptor kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.5791 | 22.4940 | AID1424908 |
Probable ATP-dependent RNA helicase DDX6 | Homo sapiens (human) | Kd | 30.0000 | 4.1030 | 4.1030 | 4.1030 | AID1424977 |
Mitogen-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.4300 | 5.2743 | 9.8000 | AID1425061 |
MAP/microtubule affinity-regulating kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 3.9689 | 58.2400 | AID1425069 |
Deoxycytidine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.0875 | 2.1630 | AID1424970 |
Mitogen-activated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.7441 | 7.3000 | AID1425056 |
Ephrin type-A receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.0752 | 8.1980 | AID1424988 |
Ephrin type-B receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 3.1536 | 53.1980 | AID1424992 |
Non-receptor tyrosine-protein kinase TYK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.5575 | 8.7000 | AID1425207 |
Wee1-like protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 3.5389 | 65.1580 | AID1425210 |
Heme oxygenase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.1190 | 0.1190 | 0.1190 | AID1425018 |
DnaJ homolog subfamily A member 1 | Homo sapiens (human) | Kd | 30.0000 | 0.9620 | 0.9620 | 0.9620 | AID1424980 |
RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0621 | 4.4000 | AID1424910 |
RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0021 | 1.6196 | 8.7000 | AID1424911 |
DNA replication licensing factor MCM4 | Homo sapiens (human) | Kd | 30.0000 | 0.6290 | 0.6290 | 0.6290 | AID1425072 |
Myosin-10 | Homo sapiens (human) | Kd | 30.0000 | 0.2290 | 0.4935 | 0.7580 | AID1425079 |
Dual specificity mitogen-activated protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 1.6429 | 9.6000 | AID1425039 |
Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 0.9559 | 9.9000 | AID1425006 |
Bone morphogenetic protein receptor type-1A | Homo sapiens (human) | Kd | 30.0000 | 0.0600 | 1.5010 | 7.0000 | AID1424921 |
Activin receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.5110 | 15.2580 | AID1424901 |
TGF-beta receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.2785 | 9.6000 | AID1425196 |
TGF-beta receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0800 | 1.8351 | 6.9000 | AID1425197 |
Tyrosine-protein kinase CSK | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 3.4578 | 39.5530 | AID1424960 |
Glycine--tRNA ligase | Homo sapiens (human) | Kd | 30.0000 | 0.0400 | 0.0400 | 0.0400 | AID1425010 |
Protein kinase C iota type | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 9.3316 | 51.0180 | AID1425133 |
Exosome RNA helicase MTR4 | Homo sapiens (human) | Kd | 30.0000 | 2.6070 | 2.6070 | 2.6070 | AID1425168 |
Tyrosine-protein kinase Tec | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.0095 | 8.7000 | AID1425193 |
Tyrosine-protein kinase ABL2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1249 | 14.9240 | AID1424891 |
Tyrosine-protein kinase FRK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.2424 | 10.8370 | AID1425007 |
G protein-coupled receptor kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 1.1890 | 1.4020 | 1.6150 | AID1425012 |
Tyrosine-protein kinase SYK | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 2.0052 | 9.2260 | AID1425188 |
26S proteasome regulatory subunit 6B | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 0.0050 | 0.0050 | AID1425141 |
Mitogen-activated protein kinase 8 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 2.0965 | 26.0590 | AID1425063 |
Mitogen-activated protein kinase 9 | Homo sapiens (human) | Kd | 2.8560 | 0.0020 | 1.4596 | 8.1000 | AID1425064 |
Dual specificity mitogen-activated protein kinase kinase 4 | Homo sapiens (human) | Kd | 1.2510 | 0.0038 | 1.6264 | 9.9000 | AID1425041 |
Dual specificity mitogen-activated protein kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.0462 | 6.6000 | AID1425040 |
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha | Homo sapiens (human) | Kd | 0.2080 | 0.2080 | 3.6125 | 7.0170 | AID1425113 |
Casein kinase I isoform alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 2.5756 | 19.3520 | AID1424961 |
Casein kinase I isoform delta | Homo sapiens (human) | Kd | 30.0000 | 0.0150 | 2.2270 | 18.3960 | AID1424962 |
MAP kinase-activated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0274 | 14.7420 | AID1425065 |
Elongation factor Tu, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.4640 | 0.4640 | 0.4640 | AID1425206 |
Choline-phosphate cytidylyltransferase A | Homo sapiens (human) | Kd | 30.0000 | 0.0410 | 0.0410 | 0.0410 | AID1425103 |
Casein kinase I isoform epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.4086 | 12.4090 | AID1424963 |
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.6890 | 1.6890 | 1.6890 | AID1424894 |
Dual specificity protein kinase CLK1 | Homo sapiens (human) | Kd | 0.2760 | 0.0020 | 1.8791 | 29.8810 | AID1424955 |
Dual specificity protein kinase CLK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.1384 | 6.5000 | AID1424956 |
Dual specificity protein kinase CLK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.4499 | 9.0000 | AID1424957 |
Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 2.4754 | 22.5430 | AID1425013 |
Glycogen synthase kinase-3 beta | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.0057 | 6.1680 | AID1425014 |
Cyclin-dependent kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.6783 | 7.7000 | AID1424949 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | Kd | 9.4920 | 0.0010 | 1.6166 | 9.9010 | AID1424950 |
Ras-related protein Rab-27A | Homo sapiens (human) | Kd | 30.0000 | 4.4930 | 4.4930 | 4.4930 | AID1425149 |
Interleukin-1 receptor-associated kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0061 | 1.5252 | 8.5000 | AID1425027 |
Ribosomal protein S6 kinase alpha-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 2.8896 | 37.6050 | AID1425160 |
Serine/threonine-protein kinase Nek2 | Homo sapiens (human) | Kd | 30.0000 | 0.1100 | 1.5649 | 6.5000 | AID1425086 |
Serine/threonine-protein kinase Nek3 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.9368 | 38.0880 | AID1425087 |
Dual specificity mitogen-activated protein kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0034 | 2.3943 | 6.5000 | AID1425043 |
LIM domain kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.7840 | 21.0890 | AID1425035 |
LIM domain kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.9717 | 52.0560 | AID1425036 |
Mitogen-activated protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.6354 | 5.9000 | AID1425057 |
Tyrosine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | 3.3160 | 3.3160 | 3.3160 | AID1425211 |
5'-AMP-activated protein kinase subunit gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.4681 | 10.2120 | AID1425126 |
Ephrin type-B receptor 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0069 | 2.1713 | 6.4100 | AID1424993 |
Ephrin type-A receptor 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.2100 | 5.9000 | AID1424990 |
Ephrin type-B receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.1678 | 26.3990 | AID1424994 |
Ephrin type-A receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 3.1525 | 43.9420 | AID1424989 |
Adenylate kinase 2, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.0360 | 1.0360 | 1.0360 | AID1424909 |
Adenosine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.8368 | 3.4930 | AID1424907 |
Ras-related protein Rab-10 | Homo sapiens (human) | Kd | 30.0000 | 1.3480 | 1.3480 | 1.3480 | AID1425148 |
Actin-related protein 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0360 | 2.7735 | 5.5110 | AID1424899 |
Actin-related protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 0.0040 | 0.0040 | AID1424898 |
GTP-binding nuclear protein Ran | Homo sapiens (human) | Kd | 30.0000 | 0.7590 | 0.7590 | 0.7590 | AID1425153 |
Casein kinase I isoform gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0460 | 1.4506 | 6.6000 | AID1424965 |
Cyclin-dependent kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 3.0602 | 63.6140 | AID1424945 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | Kd | 0.0760 | 0.0320 | 1.2007 | 3.3560 | AID1424948 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0430 | 1.3757 | 8.3000 | AID1424947 |
Cyclin-dependent kinase 16 | Homo sapiens (human) | Kd | 2.7780 | 0.0011 | 1.5855 | 10.0000 | AID1424941 |
Cyclin-dependent kinase 17 | Homo sapiens (human) | Kd | 1.2720 | 0.0010 | 0.8233 | 5.6000 | AID1424942 |
ATP-dependent 6-phosphofructokinase, platelet type | Homo sapiens (human) | Kd | 30.0000 | 0.9830 | 0.9830 | 0.9830 | AID1425108 |
Dual specificity mitogen-activated protein kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1386 | 8.7730 | AID1425038 |
DNA topoisomerase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.1480 | 1.2270 | 2.5970 | AID1425203 |
Protein kinase C theta type | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.6140 | 7.2000 | AID1425134 |
Activin receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.4853 | 16.1210 | AID1424900 |
Macrophage-stimulating protein receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.0718 | 8.4000 | AID1425078 |
Focal adhesion kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.2255 | 13.0390 | AID1425142 |
Protein kinase C delta type | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1261 | 9.2060 | AID1425131 |
Tyrosine-protein kinase BTK | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.5299 | 10.1530 | AID1424925 |
Cyclin-dependent kinase 18 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 1.4941 | 8.4000 | AID1424943 |
Activated CDC42 kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.7138 | 9.6000 | AID1425201 |
Epithelial discoidin domain-containing receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6314 | 71.4840 | AID1424972 |
Mitogen-activated protein kinase kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 1.4681 | 14.0430 | AID1425052 |
Tyrosine-protein kinase Mer | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7055 | 6.8000 | AID1425075 |
Serine/threonine-protein kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.7120 | 25.9020 | AID1425185 |
5'-AMP-activated protein kinase catalytic subunit alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0037 | 1.8913 | 15.3890 | AID1425122 |
Dual specificity mitogen-activated protein kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.6590 | 65.6770 | AID1425042 |
Mitogen-activated protein kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0420 | 2.0073 | 9.9000 | AID1425062 |
Serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.8602 | 17.5260 | AID1425182 |
Mitogen-activated protein kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.5995 | 12.4730 | AID1425044 |
Integrin-linked protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0200 | 0.4603 | 1.3290 | AID1425024 |
Rho-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7555 | 13.4620 | AID1425157 |
Non-receptor tyrosine-protein kinase TNK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.0064 | 11.2690 | AID1425200 |
Calcium/calmodulin-dependent protein kinase type II subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.0209 | 7.8000 | AID1424929 |
Calcium/calmodulin-dependent protein kinase type II subunit delta | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5044 | 20.3010 | AID1424928 |
Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.1016 | 40.2910 | AID1424981 |
Activin receptor type-2B | Homo sapiens (human) | Kd | 30.0000 | 0.0076 | 2.7328 | 9.9000 | AID1424902 |
Bone morphogenetic protein receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0190 | 2.5917 | 14.3770 | AID1424923 |
Protein-tyrosine kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0043 | 1.7430 | 9.0000 | AID1425144 |
cGMP-dependent protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 0.7072 | 3.8000 | AID1425138 |
Cyclin-dependent kinase 13 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.2571 | 4.5180 | AID1424940 |
Inhibitor of nuclear factor kappa-B kinase subunit epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.1093 | 8.3000 | AID1425023 |
Protein-tyrosine kinase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.9450 | 30.4140 | AID1425143 |
Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 2.2835 | 29.9330 | AID1425074 |
Serine/threonine-protein kinase 38 | Homo sapiens (human) | Kd | 30.0000 | 0.0560 | 1.5651 | 9.4000 | AID1425183 |
Ephrin type-A receptor 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.4445 | 6.5000 | AID1424991 |
Delta(24)-sterol reductase | Homo sapiens (human) | Kd | 30.0000 | 0.4320 | 0.4320 | 0.4320 | AID1424978 |
Ribosomal protein S6 kinase alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 2.5286 | 22.7260 | AID1425159 |
Dual specificity testis-specific protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 1.7568 | 5.6000 | AID1425194 |
Myosin light chain kinase, smooth muscle | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2088 | 7.9000 | AID1425081 |
Mitogen-activated protein kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.4610 | 3.7430 | AID1425058 |
Serine/threonine-protein kinase STK11 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.9949 | 5.9000 | AID1425178 |
Serine/threonine-protein kinase N1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 3.1729 | 49.8130 | AID1425117 |
Serine/threonine-protein kinase N2 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.7527 | 9.9000 | AID1425118 |
Mitogen-activated protein kinase 14 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 0.5036 | 8.5000 | AID1425059 |
Calcium/calmodulin-dependent protein kinase type IV | Homo sapiens (human) | Kd | 30.0000 | 0.0300 | 1.9215 | 5.4600 | AID1424930 |
Mitogen-activated protein kinase kinase kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.5639 | 17.9840 | AID1425045 |
Discoidin domain-containing receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.9888 | 42.2800 | AID1424973 |
AP2-associated protein kinase 1 | Homo sapiens (human) | Kd | 4.2160 | 0.0012 | 1.3707 | 13.7110 | AID1424889 |
Myosin light chain kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6184 | 10.4240 | AID1425082 |
Uncharacterized aarF domain-containing protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.4990 | 0.7960 | AID1424906 |
Putative heat shock protein HSP 90-beta 2 | Homo sapiens (human) | Kd | 30.0000 | 2.5660 | 2.5660 | 2.5660 | AID1425019 |
Rab-like protein 3 | Homo sapiens (human) | Kd | 30.0000 | 4.8300 | 4.8300 | 4.8300 | AID1425151 |
Serine/threonine-protein kinase MRCK alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.5547 | 14.0200 | AID1424933 |
Serine/threonine-protein kinase MRCK gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0370 | 1.9625 | 9.5000 | AID1424935 |
Acyl-CoA dehydrogenase family member 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0780 | 1.6997 | 3.9570 | AID1424892 |
Serine/threonine-protein kinase N3 | Homo sapiens (human) | Kd | 30.0000 | 0.0990 | 0.7365 | 1.3740 | AID1425119 |
Serine/threonine-protein kinase ULK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 1.3350 | 9.9000 | AID1425209 |
Uncharacterized protein FLJ45252 | Homo sapiens (human) | Kd | 27.3340 | 0.0030 | 1.2292 | 9.3110 | AID1425147 |
Acyl-CoA dehydrogenase family member 11 | Homo sapiens (human) | Kd | 30.0000 | 1.9160 | 3.0730 | 4.1470 | AID1424893 |
Serine/threonine-protein kinase/endoribonuclease IRE2 | Homo sapiens (human) | Kd | 30.0000 | 0.1160 | 0.7604 | 1.5000 | AID1424998 |
Serine/threonine-protein kinase MARK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.8425 | 11.1030 | AID1425068 |
Serine/threonine-protein kinase TAO1 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 2.1612 | 18.7570 | AID1425189 |
STE20-related kinase adapter protein alpha | Homo sapiens (human) | Kd | 30.0000 | 0.3160 | 1.7208 | 3.6720 | AID1425186 |
AarF domain-containing protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0230 | 3.1137 | 22.7470 | AID1424904 |
Mitogen-activated protein kinase kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.6413 | 15.4350 | AID1425053 |
MAP kinase-activated protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 1.1241 | 3.1180 | AID1425067 |
Misshapen-like kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.1425 | 8.9000 | AID1425077 |
Atypical kinase COQ8A, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 5.1673 | 65.3020 | AID1424905 |
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Homo sapiens (human) | Kd | 1.7210 | 0.0030 | 2.7522 | 8.8000 | AID1425115 |
Mitogen-activated protein kinase 15 | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 0.6880 | 4.5000 | AID1425060 |
Serine/threonine-protein kinase Nek9 | Homo sapiens (human) | Kd | 30.0000 | 0.0160 | 2.7428 | 19.6170 | AID1425089 |
ATP-dependent RNA helicase DDX1 | Homo sapiens (human) | Kd | 30.0000 | 0.0860 | 0.0860 | 0.0860 | AID1424974 |
Mitogen-activated protein kinase kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.9378 | 5.5000 | AID1425051 |
Aurora kinase B | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.0614 | 22.8520 | AID1424918 |
MAP/microtubule affinity-regulating kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0054 | 1.1029 | 4.9000 | AID1425070 |
Serine/threonine-protein kinase Nek1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 2.4294 | 8.3000 | AID1425085 |
PAS domain-containing serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 1.0670 | 1.0670 | 1.0670 | AID1425102 |
Calcium/calmodulin-dependent protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.2331 | 52.8470 | AID1424931 |
EKC/KEOPS complex subunit TP53RK | Homo sapiens (human) | Kd | 30.0000 | 0.3110 | 1.9519 | 3.8400 | AID1425204 |
Dual specificity testis-specific protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 0.0020 | 0.0020 | AID1425195 |
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0440 | 0.9285 | 2.9000 | AID1425116 |
Mitogen-activated protein kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0700 | 6.5647 | 50.5360 | AID1425049 |
Mitogen-activated protein kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.5331 | 9.9000 | AID1425047 |
Eukaryotic translation initiation factor 2-alpha kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0580 | 1.9224 | 4.8360 | AID1424984 |
Nucleolar GTP-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0090 | 4.1035 | 8.1980 | AID1425016 |
Serine/threonine-protein kinase D2 | Homo sapiens (human) | Kd | 5.6230 | 0.0081 | 2.3723 | 25.0190 | AID1425136 |
NUAK family SNF1-like kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.6774 | 4.6000 | AID1425095 |
RNA cytidine acetyltransferase | Homo sapiens (human) | Kd | 30.0000 | 1.2400 | 1.2400 | 1.2400 | AID1425083 |
Serine/threonine-protein kinase SIK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.8165 | 41.7950 | AID1425166 |
STE20-like serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.8573 | 99.2320 | AID1425171 |
Serine/threonine-protein kinase TAO3 | Homo sapiens (human) | Kd | 15.8520 | 0.0002 | 2.7131 | 14.1960 | AID1425191 |
dCTP pyrophosphatase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.5730 | 1.7403 | 3.0540 | AID1424971 |
Dual specificity protein kinase CLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4122 | 8.3000 | AID1424958 |
Casein kinase I isoform gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0530 | 2.0622 | 5.7000 | AID1424964 |
Serine/threonine-protein kinase PAK 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 1.9194 | 9.7000 | AID1425101 |
Phenylalanine--tRNA ligase beta subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0045 | 0.0060 | AID1425000 |
Isoleucine--tRNA ligase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 0.0110 | 0.0110 | AID1425020 |
BMP-2-inducible protein kinase | Homo sapiens (human) | Kd | 26.4660 | 0.0022 | 2.4097 | 56.0320 | AID1424920 |
Interleukin-1 receptor-associated kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 3.4719 | 34.1450 | AID1425029 |
Mitogen-activated protein kinase kinase kinase 20 | Homo sapiens (human) | Kd | 30.0000 | 0.0023 | 1.7034 | 13.6380 | AID1425213 |
Cyclin-dependent kinase 12 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.8032 | 5.6350 | AID1424939 |
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 | Homo sapiens (human) | Kd | 30.0000 | 3.9200 | 3.9200 | 3.9200 | AID1425084 |
Serine/threonine-protein kinase pim-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0019 | 0.8415 | 5.0000 | AID1425112 |
Serine/threonine-protein kinase 26 | Homo sapiens (human) | Kd | 30.0000 | 0.0074 | 1.7380 | 8.3000 | AID1425181 |
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 0.0070 | 0.0070 | AID1425187 |
Serine/threonine-protein kinase NLK | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.0226 | 4.4000 | AID1425090 |
5'-AMP-activated protein kinase subunit gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 1.1581 | 9.1280 | AID1425127 |
Serine/threonine-protein kinase TBK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.7674 | 49.6010 | AID1425192 |
Septin-9 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 0.2430 | 0.6350 | AID1425165 |
Ribosomal protein S6 kinase alpha-6 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 2.4153 | 23.7620 | AID1425163 |
TRAF2 and NCK-interacting protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0047 | 1.3935 | 10.0000 | AID1425199 |
Serine/threonine-protein kinase TAO2 | Homo sapiens (human) | Kd | 27.9730 | 0.0100 | 2.0176 | 12.9420 | AID1425190 |
Long-chain-fatty-acid--CoA ligase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 0.6353 | 1.6900 | AID1424897 |
Serine/threonine-protein kinase ICK | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.4717 | 9.3000 | AID1425021 |
RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.7646 | 6.2000 | AID1424912 |
Serine/threonine-protein kinase 38-like | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 1.4692 | 6.9000 | AID1425184 |
Serine/threonine-protein kinase SIK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.5086 | 10.3180 | AID1425167 |
Mitogen-activated protein kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0024 | 1.3298 | 6.9000 | AID1425046 |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 1.8129 | 9.5000 | AID1424982 |
Mitogen-activated protein kinase kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.9494 | 50.2140 | AID1425055 |
Receptor-interacting serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.4797 | 6.7000 | AID1425156 |
Serine/threonine-protein kinase MRCK beta | Homo sapiens (human) | Kd | 30.0000 | 0.0340 | 3.6252 | 50.0050 | AID1424934 |
Interleukin-1 receptor-associated kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.7137 | 25.5810 | AID1425028 |
Serine/threonine-protein kinase 24 | Homo sapiens (human) | Kd | 30.0000 | 0.0065 | 0.8920 | 4.0840 | AID1425180 |
Casein kinase I isoform gamma-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.3978 | 8.7000 | AID1424966 |
Mitogen-activated protein kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0390 | 2.3970 | 8.4000 | AID1425048 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4 | Navigating the kinome. |
AID1125319 | Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1424941 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1846041 | Antitumor activity against human Med-211 FH cells xenografted in athymic nude mouse assessed as tumor regression at 75 mg/kg, po QD for 28 days | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762692 | Inhibition of CDK6/Cyclin D3 (unknown origin) at 20 nM using ATP by mobility shift assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID526644 | Inhibition of CDK4 | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638154 | Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay | |||
AID1425129 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1824403 | Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1785354 | Synergistic antiproliferative activity against human A549 cells assessed as combination index in presence of 2.5 to 46 uM tubastatin-A by Chou-Talalay method | |||
AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438427 | Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1069211 | Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase at 0.5 to 1 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1543671 | Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. |
AID1438442 | Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1613045 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents. |
AID240730 | Inhibition of Cyclin dependent kinase 2-cyclin A | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
AID1424982 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424915 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1737179 | Cell cycle arrest in human COLO 205 cells assessed as accumulation at G0/G1 phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry relative to control | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1824398 | Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1125297 | Inhibition of GST-fused human FLT3 cytoplasmic domain (amino acids 564 to 993) using Ulight-JAK1 as substrate after 1 hr by TR-FRET assay | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1424894 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438412 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 0.04 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 1.99%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1317302 | Inhibition of CDK2/cyclin A (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762719 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 1.5 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 21.7%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1551224 | Oral bioavailability in human at 125 mg | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1544225 | Induction of CRBN-mediated CDK4 degradation in human MIAPaCa2 cells measured after 4 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Selective degradation of CDK6 by a palbociclib based PROTAC. |
AID1762682 | Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1917240 | Inhibition of CDK4/cyclin D1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762684 | Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1425074 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638151 | Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells at 10 uM using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay relative to control | |||
AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1893763 | Growth inhibition of human LNCaP/AR cells assessed as decrease in tumor spheroid growth at 30 nM with media replenishment twice per week along with 3 to 4-day interval compound relative to control | 2022 | ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9 | Combination of Cyclin-Dependent Kinase 4 Inhibitors and Androgen Receptor Inhibitors as Cancer Therapy. |
AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648295 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2/M phase at 20 uM measured after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 15.9%) | |||
AID1762685 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1648310 | Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 20 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (0.877%) | |||
AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1846042 | Antitumor activity against human Med-1712FH cells xenografted in athymic nude mouse assessed as tumor regression at 75 mg/kg, po QD for 28 days | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1849047 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | |||
AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1467205 | Cell cycle arrest in human ALL5 cells assessed as accumulation at G2 phase at 1 uM after 72 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 19.1%) | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Activity of resveratrol triesters against primary acute lymphoblastic leukemia cells. |
AID1425184 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID767467 | Inhibition of JAK3 (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Selectivity data: assessment, predictions, concordance, and implications. |
AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425061 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438431 | Growth inhibition of human M229 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438421 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 0.40 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 61.01%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1613047 | Inhibition of human full length N-terminal GST-tagged CDK6 (1 to 326 end residues)/CyclinD3 (1 to 292 end residues) expressed in baculovirus expression system at 1 uM using FAM-labelled peptide as substrate preincubated for 10 mins followed by substrate a | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents. |
AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425115 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638155 | Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay | |||
AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1283433 | Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATP | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
AID526663 | Inhibition of CDK6 | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
AID240709 | Inhibition of Cyclin-dependent kinase 4-cyclinD | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
AID1762713 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 0.375 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 21.7%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1438433 | Growth inhibition of human M249 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID442994 | Inhibition of CDK4 | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors. |
AID1283446 | Inhibition of CDK7 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
AID1513684 | Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1425054 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069215 | Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1638158 | Inhibition of CDK6/cyclin D1 (unknown origin) using RBER-CHKtide as substrate measured after 1 hr by ADP-glo luminescence assay | |||
AID1667791 | Protac activity at CRBN/CDK6 in human Jurkat cells assessed as induction of CDK6 degradation measured after 24 hrs by capillary electrophoresis | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs. |
AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438415 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 0.04 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 17.94%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069262 | Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438420 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 0.40 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 1.99%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1648276 | Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
AID1402374 | Unbound brain to plasma concentration ratio in mouse at 1 mg/kg, iv after 5 mins | |||
AID1638153 | Inhibition of CDK6/cyclin D1 (unknown origin) at 10 uM using RBER-CHKtide as substrate measured after 1 hr by ADP-glo luminescence assay relative to control | |||
AID1283447 | Inhibition of CDK9 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
AID1438456 | Induction of apoptosis in human MV4-11 cells assessed as viable cells at GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 93.05%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1516634 | Antiproliferative activity against human JeKo1 cells after 84 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. |
AID1588586 | Efflux ratio in MDCK2 expressing mouse bcrp1 | |||
AID1395324 | Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 34.1%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1588846 | Unbound brain to plasma ratio in Sprague-Dawley rat at 30 mg/kg, po after 48 hrs by LC-MS/MS analysis | |||
AID1069213 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762720 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2 phase at 1.5 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 15.08%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1069265 | Inhibition of CDK4/cyclinD1 (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438447 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 18.11%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1125320 | Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1678844 | Inhibition of CDK4 (unknown origin) | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Online informatics resources to facilitate cancer target and chemical probe discovery. |
AID1438459 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 0.06%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1824401 | Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1125323 | Induction of apoptosis in sorafenib-resistant human MOLM13 cells harboring FLT3 ITD+D835Y mutant at 1 uM after 48 hrs by Annexin V/Sytox Green staining based flow cytometry | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425012 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1613044 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents. |
AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648275 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
AID1425211 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424508 | Inhibition of CDK4 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. |
AID1737183 | Inhibition of recombinant human full-length N-terminal GST-fused CDK4 (1 to 303 residues)/GST-tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system using ULight-elF4E-binding protein 1 peptide as substrate measured after 30 mins b | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1438428 | Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1868085 | Inhibition of CDK4/cyclin D (unknown origin) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9 | From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy. |
AID1762708 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.1875 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 54.21%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1425119 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1876017 | Antiviral activity against HIV-1 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1317299 | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1682921 | Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Synthesis and antiproliferative evaluation of novel 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives as potential anticancer agents. |
AID1613043 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents. |
AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1737230 | Inhibition of CDK7/cyclin H (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425180 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1684534 | Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 33 | Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells. |
AID1069212 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1327283 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities. |
AID1438416 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 0.20 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 1.99%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1824402 | Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762709 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 0.1875 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 21.7%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1875921 | Antiviral activity against pseudotype NL4-3 HIV-1 infected in 24 hrs pretreated monocyte-derived macrophage | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1737184 | Inhibition of human full-length N-terminal GST tagged CDK6 (1 to 326 residues)/GST-tagged cyclinD3 (1 to 292 residues) expressed in baculovirus expression system using ULight-elF4E-binding protein 1 peptide as substrate measured after 30 mins by LANCE ass | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1893765 | Growth inhibition of human LNCaP/AR cells assessed as decrease in tumor spheroid growth at 30 nM with media replenishment twice per week along with 3 to 4-day interval compound in presence of enzalutamide relative to control | 2022 | ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9 | Combination of Cyclin-Dependent Kinase 4 Inhibitors and Androgen Receptor Inhibitors as Cancer Therapy. |
AID1438446 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 21.97%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1737187 | Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648294 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 20 uM measured after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 26.45%) | |||
AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1125299 | Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1513682 | Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438438 | Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1395323 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 60.7%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1917249 | Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
AID1762710 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2 phase at 0.1875 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 15.08%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1424984 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1283430 | Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
AID1327286 | Antitumor activity against human estrogen-independent human MCF7 cells xenografted in RNU rat assessed as tumor growth inhibition at 100 mg/kg/day, ig administered for 14 days measured on day 15 | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities. |
AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438450 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 5 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 21.97%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1849050 | Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | |||
AID1438464 | Induction of apoptosis in human MV4-11 cells assessed as viable cells at 10 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 93.05%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438463 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 5 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 0.06%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1824400 | Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1069264 | Inhibition of CDK2/cyclinA (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1516629 | Antiproliferative activity against human THP1 cells after 84 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. |
AID1438465 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 10 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 2.01%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1648278 | Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
AID1638156 | Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay | |||
AID1737229 | Inhibition of CDK2/cyclin A2 (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638213 | Inhibition of CDK6/cyclin D1 (unknown origin) | |||
AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069224 | Inhibition of CDK6/cyclinD1 (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425212 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648312 | Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 20 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (0.498%) | |||
AID1239753 | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1894170 | Inhibition of CDK6 (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID1438423 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 0.40 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 17.94%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1239754 | Inhibition of CDK2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1551211 | Inhibition of CDK1 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1424937 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638149 | Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells at 10 uM using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay relative to control | |||
AID248708 | Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
AID1818825 | Cell cycle arrest in human K562 cells assessed as accumulation of cells in G1 phase at 2 uM by PI staining based flow cytometry method (Rvb = 43.94 %) | |||
AID1438432 | Growth inhibition of human M238 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1467202 | Cell cycle arrest in human ALL5 cells assessed as accumulation at subG1 phase at 1 uM after 72 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 0.54 %) | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Activity of resveratrol triesters against primary acute lymphoblastic leukemia cells. |
AID1424945 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1849068 | Induction of cell cycle arrest in human T47D cells assessed as accumulation of cells at G1 phase at 1.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 69.55 %) | |||
AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1239755 | Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1785351 | Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1849060 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation of cells at G1 phase at 2.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 57.38%) | |||
AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1737228 | Inhibition of CDK1/cyclin B (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1438462 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 5 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 4.87%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1516630 | Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. |
AID1069221 | Inhibition of FLT3 (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1516632 | Antiproliferative activity against human RPMI8226 cells after 84 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. |
AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1917241 | Inhibition of CDK6/cyclin D1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
AID1327281 | Inhibition of CDK6 (unknown origin) using histone H1 as substrate after 10 mins in presence of [gamma32P]ATP | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities. |
AID1732739 | Inhibition of human CDK4/cyclin D (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors. |
AID1425183 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1682922 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Synthesis and antiproliferative evaluation of novel 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives as potential anticancer agents. |
AID1438440 | Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1438429 | Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638212 | Inhibition of CDK9/cyclin T1 (unknown origin) | |||
AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438448 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 5 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 0.91%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425084 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1785353 | Synergistic antiproliferative activity against human A549 cells assessed as combination index in presence of vorinostat by Chou-Talalay method | |||
AID1648272 | Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay | |||
AID1551214 | Inhibition of CDK5 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425079 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438411 | Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1438409 | Inhibition of CDK9/cyclin T1 (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1785349 | Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424509 | Inhibition of CDK6 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. |
AID1917247 | Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
AID1425100 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638165 | Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay | |||
AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424972 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1682920 | Cytotoxicity against HEK293 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Synthesis and antiproliferative evaluation of novel 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives as potential anticancer agents. |
AID1424973 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID767469 | Inhibition of CDK9 (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Selectivity data: assessment, predictions, concordance, and implications. |
AID1438460 | Induction of apoptosis in human MV4-11 cells assessed as viable cells at 5 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 93.05%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1395320 | Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 50.3%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762732 | Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 40 mg/kg, po measured every 3 days for 21 days | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438410 | Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1283431 | Inhibition of CDK1 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
AID1425195 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438466 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 10 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 4.87%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID248709 | Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424994 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1395319 | Cell cycle arrest in human K562 cells assessed as accumulation at G1 phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 34.6%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1425207 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425009 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1737186 | Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1438445 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 58.99%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1917248 | Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
AID1785348 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1327282 | Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities. |
AID1425020 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425010 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438413 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 0.04 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 61.01%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1513678 | Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1424964 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425080 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1125322 | Induction of apoptosis in human MOLM13 cells harboring FLT3 ITD mutant at 1 uM after 48 hrs by Annexin V/Sytox Green staining based flow cytometry | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1818782 | Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay | |||
AID1424942 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1875922 | Antiviral activity against HSV-1 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069214 | Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1317303 | Inhibition of CDK5/p25 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1868058 | Inhibition of CDK6/Cyclin D (unknown origin) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9 | From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy. |
AID1682924 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Synthesis and antiproliferative evaluation of novel 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives as potential anticancer agents. |
AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438419 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 0.20 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 17.94%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1667798 | Inhibition of human CDK6/cyclin-D2 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs. |
AID1425090 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438404 | Inhibition of CDK4/cyclin D1 (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425095 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424957 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638167 | Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay | |||
AID1762689 | Inhibition of CDK4/Cyclin D1 (unknown origin) at 200 nM using ATP by mobility shift assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1513683 | Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1648311 | Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 20 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (2.78%) | |||
AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1894169 | Inhibition of CDK4 (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID1638150 | Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells at 10 uM using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay relative to c | |||
AID1438458 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 4.87%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638168 | Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay | |||
AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438449 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 5 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 58.99%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1467203 | Cell cycle arrest in human ALL5 cells assessed as accumulation at G1 phase at 1 uM after 72 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 64.4%) | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Activity of resveratrol triesters against primary acute lymphoblastic leukemia cells. |
AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438444 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 0.91%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1069218 | Inhibition of FGFR1 (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1785375 | Inhibition of CDK2/4/6 in human A549 cells assessed as decrease in Rb phosphorylation at 10 uM measured after 48 hrs by Western blot analysis | |||
AID1438454 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 10 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 21.97%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069210 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at sub-G1 phase at 0.5 to 1 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762714 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2 phase at 0.375 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 15.08%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1876252 | Inhibition of CDK6 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1516607 | Induction of CRBN-mediated CDK6 degradation in human U251 cells at 100 nM after 24 hrs by immunoblot analysis | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. |
AID1327279 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities. |
AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1818808 | Induction of apoptosis in human K562 cells assessed as early apoptotic cells at 2 uM by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.38%) | |||
AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438467 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 10 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 0.06%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762695 | Inhibition of CDK4/Cyclin D3 (unknown origin) by mobility shift assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069263 | Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1438407 | Inhibition of CDK2/cyclin A (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1854216 | Cytotoxicity against human mesothelioma cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Small molecules targeting cGAS-STING pathway for autoimmune disease. |
AID1317300 | Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1849048 | Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | |||
AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1513698 | Induction of cell cycle arrest in human HCT116 cells assessed as reduction in accumulation at G1 phase at 0.16 to 10 uM after 24 hrs by propidium iodide-staining based flow cytometry | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1875919 | Inhibition of CDK4 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1438455 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 10 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 18.11%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1876251 | Antiviral activity against HSV-1 assessed as inhibition of viral replication | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1667787 | Inhibition of human CDK6/cyclin-D3 using RB protein as substrate by [gamma-33P]-ATP assay | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs. |
AID1438405 | Inhibition of CDK6/cyclin D3 (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1239752 | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1125307 | Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1438461 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 5 times GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 2.01%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762715 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.75 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 54.21%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1762711 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.375 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 54.21%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1424925 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425169 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438417 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 0.20 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 61.01%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1069217 | Inhibition of ABL (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1849049 | Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | |||
AID1588587 | Efflux ratio in gMDCKI cells expressing human MDR1 | |||
AID1125306 | Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1638152 | Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells at 10 uM using RBCTF as substrate measured after 1 hr by ADP-glo lumine | |||
AID1551226 | Protein binding in human plasma at 125 mg, po | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1785350 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1638157 | Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as | |||
AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1785347 | Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | |||
AID1438435 | Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424951 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1613046 | Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents. |
AID1849071 | Induction of cell cycle arrest in human T47D cells assessed as accumulation of cells at G2 phase at 1.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 16.57%) | |||
AID1438434 | Growth inhibition of human M249R cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1768217 | Antitumor activity against human MCF7 cells xenografted in nude mouse assessed as reduction in tumor growth at 50 mg/kg, po administered once daily for 26 days by calipers method relative to control | |||
AID1551213 | Inhibition of CDK4 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1425072 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425109 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438457 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at GI50 after 24 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 2.01%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438437 | Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1438406 | Inhibition of CDK1/cyclin B (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1648277 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
AID1425041 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424943 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1513680 | Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1425034 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424918 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648309 | Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 20 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (95.8%) | |||
AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425189 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1824399 | Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1069219 | Inhibition of PDGFRbeta (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424936 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1728101 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved? |
AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648274 | Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay | |||
AID1638166 | Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay | |||
AID1513679 | Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1125295 | Inhibition of CDK4/cyclin D1 (unknown origin) using Rb as substrate after 60 mins by scintillation counting analysis in presence of [r-33P]ATP | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1737182 | Inhibition of CDK9/cyclin T1 (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648293 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 20 uM measured after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 57.65%) | |||
AID1516633 | Antiproliferative activity against human HL60 cells after 84 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. |
AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1551225 | Tmax in human at 125 mg, po | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1425199 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438414 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 0.04 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 19.07%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069208 | Induction of apoptosis in human MCF7 cells assessed as PARP cleavage at 1 to 10 uM after 24 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1917246 | Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425137 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438436 | Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1543670 | Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. |
AID1438430 | Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1551215 | Inhibition of CDK6 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1762683 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425038 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762690 | Inhibition of CDK4/Cyclin D1 (unknown origin) at 20 nM using ATP by mobility shift assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1424948 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762717 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2 phase at 0.75 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 15.08%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1438408 | Inhibition of CDK7/cyclin H (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1513706 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 0.16 to 10 uM after 24 hrs by propidium iodide-staining based flow cytometry relative to control | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1818809 | Induction of apoptosis in human K562 cells assessed as assessed as late apoptotic cells at 2 uM by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.07%) | |||
AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1283429 | Inhibition of CDK4 (unknown origin) | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases. |
AID1638210 | Inhibition of CDK2/cyclin A2 (unknown origin) | |||
AID1424906 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438439 | Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1638209 | Inhibition of CDK4/cyclin D1 (unknown origin) | |||
AID1327280 | Inhibition of CDK4 (unknown origin) using histone H1 as substrate after 10 mins in presence of [gamma32P]ATP | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities. |
AID1069222 | Inhibition of FYN (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1317304 | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1467204 | Cell cycle arrest in human ALL5 cells assessed as accumulation at S phase at 1 uM after 72 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 15.2%) | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Activity of resveratrol triesters against primary acute lymphoblastic leukemia cells. |
AID1425154 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1818810 | Induction of apoptosis in human K562 cells assessed as assessed as necrotic cells at 2 uM by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.61%) | |||
AID1425042 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1395318 | Cell cycle arrest in human K562 cells assessed as accumulation at sub G1 phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 15%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424931 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1513681 | Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1818783 | Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay | |||
AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425073 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425122 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1876096 | Cytotoxicity against human MDM cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762718 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 1.5 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 54.21%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1849041 | Inhibition of CDK6/cyclin-D1 (unknown origin) in presence of ATP by time resolved-FRET assay | |||
AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1239756 | Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1125321 | Induction of apoptosis in human U937 cells harboring wild type FLT3 at 1 uM after 48 hrs by Annexin V/Sytox Green staining based flow cytometry | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1069225 | Inhibition of CDK4/cyclinD1 (unknown origin) using retinoblastoma as substrate after 30 mins by autoradiography in presence of [gamma-32P]ATP | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1069220 | Inhibition of FMS (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1516631 | Antiproliferative activity against human Mino cells after 84 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. |
AID1732688 | Inhibition of CDK2/cyclin A2 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors. |
AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424975 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1543657 | Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. |
AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1543686 | Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. |
AID1876285 | Inhibition of CDK4 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1613042 | Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents. |
AID1762691 | Inhibition of CDK6/Cyclin D3 (unknown origin) at 200 nM using ATP by mobility shift assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1638211 | Inhibition of CDK1/cyclin B1 (unknown origin) | |||
AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1395325 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.3%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1125298 | Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. |
AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1667790 | Protac activity at CRBN/CDK4 in human Jurkat cells assessed as induction of CDK4 degradation measured after 24 hrs by capillary electrophoresis | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs. |
AID1438443 | Effect on total Rb protein levels in human MV4-11 cells at GI50 after 12 to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1818807 | Induction of apoptosis in human K562 cells assessed as viable cells at 2 uM by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 93.9%) | |||
AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1875920 | Inhibition of CDK6 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424983 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1824378 | Inhibition of CDK6/Cyclin D1 (unknown origin) using ULight-MBP peptide substrate in presence of ATP by TR-FRET assay | |||
AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1762716 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 0.75 uM after 12 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 21.7%) | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1682923 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Synthesis and antiproliferative evaluation of novel 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives as potential anticancer agents. |
AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438452 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 10 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 0.91%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1069216 | Inhibition of PI3Kdelta (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1737185 | Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1438453 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 10 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 58.99%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1424899 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438451 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 5 times GI50 after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 18.11%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1667786 | Inhibition of human CDK4/cyclin-D1 using RB protein as substrate by [gamma-33P]-ATP assay | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs. |
AID1425167 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1395321 | Cell cycle arrest in human K562 cells assessed as accumulation at G2/M phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 15%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1849064 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation of cells at G2 phase at 2.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 29.66%) | |||
AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1438418 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 0.20 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 19.07%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1551212 | Inhibition of CDK2 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1395322 | Cell cycle arrest in human MCF7 cells assessed as accumulation at sub G1 phase at 0.25 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 7.1%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines. |
AID1876250 | Antiviral activity against HIV-1 assessed as inhibition of viral replication | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1762694 | Inhibition of CDK6/Cyclin D3 (unknown origin) by mobility shift assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. |
AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1544224 | Induction of CRBN-mediated CDK6 degradation in human MIAPaCa2 cells measured after 4 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Selective degradation of CDK6 by a palbociclib based PROTAC. |
AID1818784 | Antiproliferative activity against AML patient derived mononuclear cells of assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay | |||
AID1069223 | Inhibition of ARK5 (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1438422 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 0.40 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 19.07%) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. |
AID1893761 | Growth inhibition of human LNCaP/AR cells assessed as decrease in tumor spheroid growth at 100 nM with media replenishment twice per week along with 3 to 4-day interval compound relative to control | 2022 | ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9 | Combination of Cyclin-Dependent Kinase 4 Inhibitors and Androgen Receptor Inhibitors as Cancer Therapy. |
AID1069206 | Induction of apoptosis in human MDA-MB-231 cells assessed as PARP cleavage at 1 to 10 uM after 24 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). |
AID1648273 | Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay | |||
AID1425075 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425158 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1667797 | Inhibition of human CDK4/cyclin-D1 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs. |
AID1424968 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1402379 | Inhibition of CDK6/Cyclin-D3 (unknown origin) using histoneH1 as substrate after 90 mins by ADP-Glo assay | |||
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1795873 | CDKs Assay from Article 10.1021/jm049354h: \\Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.\\ | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1345613 | Human cyclin dependent kinase 6 (CDK4 subfamily) | 2004 | Molecular cancer therapeutics, Nov, Volume: 3, Issue:11 | Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. |
AID1345601 | Human cyclin dependent kinase 4 (CDK4 subfamily) | 2004 | Molecular cancer therapeutics, Nov, Volume: 3, Issue:11 | Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Toward understanding the structural basis of cyclin-dependent kinase 6 specific inhibition. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Toward understanding the structural basis of cyclin-dependent kinase 6 specific inhibition. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 16 (1.78) | 29.6817 |
2010's | 481 (53.56) | 24.3611 |
2020's | 401 (44.65) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (77.81) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 126 (13.83%) | 5.53% |
Reviews | 121 (13.28%) | 6.00% |
Case Studies | 54 (5.93%) | 4.05% |
Observational | 14 (1.54%) | 0.25% |
Other | 596 (65.42%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
A Randomized Trial of Neratinib, A Pan-ERBB Inhibitor, Alone or in Combination With Palbociclib, a CDK4/6 Inhibitor, in Patients With HER2+ Gynecologic Cancers and Other Solid Tumors: A ComboMATCH Treatment Trial [NCT06126276] | Phase 2 | 70 participants (Anticipated) | Interventional | 2024-02-20 | Not yet recruiting | ||
Phase II Pilot, Prospective, Open Label, Multicenter CT, to Evaluate the Safety and Efficacy of Palbociclib (PD0332991), a Cyclin-dependent Kinase 4 and 6 (CDK4 and CDK6) Inhibitor, in Patients With Oligodendroglioma or Recurrent Oligoastrocytoma Anaplast [NCT02530320] | Phase 2 | 40 participants (Actual) | Interventional | 2015-10-25 | Completed | ||
A Phase III Randomized, Open-Label Study Evaluating Efficacy and Safety of Giredestrant Compared With Fulvestrant, Both Combined With a CDK4/6 Inhibitor, in Patients With Estrogen Receptor-Positive, HER2-Negative Advanced Breast Cancer With Resistance to [NCT06065748] | Phase 3 | 1,050 participants (Anticipated) | Interventional | 2023-12-11 | Recruiting | ||
Phase 2a Study of ZW25 in Combination With Palbociclib Plus Fulvestrant [NCT04224272] | Phase 2 | 51 participants (Actual) | Interventional | 2020-06-10 | Active, not recruiting | ||
Molecular Analysis for Therapy Choice (MATCH) [NCT02465060] | Phase 2 | 6,452 participants (Anticipated) | Interventional | 2015-08-17 | Active, not recruiting | ||
Phase I Trial of PD 0332991 Plus Bortezomib in Patients With Relapsed Mantle Cell Lymphoma [NCT01111188] | Phase 1 | 20 participants (Actual) | Interventional | 2010-08-23 | Terminated | ||
European Treatment Patterns and Outcomes Associated With First-Line CDK4/6 Inhibition and Hormonal Therapies Assessed in a Real-World Non-Interventional Study (EUCHARIS) [NCT05043506] | 2,400 participants (Anticipated) | Observational | 2022-02-08 | Recruiting | |||
A Phase II Study of Palbociclib (PD-0332991) in Combination With Ibrutinib in Patients With Previously Treated Mantle Cell Lymphoma [NCT03478514] | Phase 2 | 39 participants (Actual) | Interventional | 2018-09-11 | Active, not recruiting | ||
Phase II Trial of Primary Endocrine Therapy With Combination of Fulvestrant or an Aromatase Inhibitor and Palbociclib in Elderly Patients With Hormone Responsive Breast Cancer Who Have Inoperable Tumor Or Operable Tumor But Cannot Undergo Surgery Due to F [NCT02760030] | Phase 2 | 37 participants (Anticipated) | Interventional | 2017-02-16 | Recruiting | ||
A MULTICENTER, RANDOMIZED, DOUBLE-BLIND PHASE 3 STUDY OF PALBOCICLIB (ORAL CDK 4/6 INHIBITOR) PLUS LETROZOLE VERSUS PLACEBO PLUS LETROZOLE FOR THE TREATMENT OF PREVIOUSLY UNTREATED ASIAN POSTMENOPAUSAL WOMEN WITH ER (+), HER2 (-) ADVANCED BREAST CANCER [NCT02297438] | Phase 3 | 340 participants (Actual) | Interventional | 2015-03-23 | Active, not recruiting | ||
ctDNA-guided Adaptive Therapy Escalation in ER+ MBC: A Phase 1b Study With Letrozole, Palbociclib and Onapristone ER [NCT04872608] | Phase 1 | 0 participants (Actual) | Interventional | 2021-09-09 | Withdrawn(stopped due to The sponsor closed the study due to discontinuing their onapristone program) | ||
A Randomized Study Evaluating the Safety and Effects of the Combination of Palbociclib With Epirubicin and Cyclophosphamide Followed by Paclitaxel as Neoadjuvant Therapy in Triple Negative Breast Cancer [NCT03756090] | 100 participants (Anticipated) | Interventional | 2018-12-01 | Not yet recruiting | |||
Randomized, Non-comparative Neoadjuvant Phase II Study in Patients With ER+/HER2- Breast Cancer >= 2 cm With Safety Run-in, Assessing Nivolumab + Palbociclib + Anastrozole [NCT04075604] | Phase 2 | 23 participants (Actual) | Interventional | 2019-10-18 | Completed | ||
A Biomarker-Driven Master Protocol for Previously Treated Squamous Cell Lung Cancer (Lung-Map) [NCT02154490] | 1,864 participants (Actual) | Observational | 2014-07-08 | Completed | |||
A Phase I/II Study of Palbociclib, Letrozole and T-DM1 in Trastuzumab Refractory Estrogen Receptor Positive (ER+) and HER2 Positive Metastatic Breast Cancer [NCT03709082] | Phase 1/Phase 2 | 3 participants (Actual) | Interventional | 2018-10-15 | Active, not recruiting | ||
A RANDOMIZED, MULTICENTER, DOUBLE-BLIND PHASE 2 STUDY OF PALBOCICLIB PLUS CETUXIMAB VERSUS CETUXIMAB FOR THE TREATMENT OF HUMAN PAPILLOMAVIRUS-NEGATIVE, CETUXIMAB-NAÏVE PATIENTS WITH RECURRENT/METASTATIC SQUAMOUS CELL CARCINOMA OF THE HEAD AND NECK AFTER [NCT02499120] | Phase 2 | 125 participants (Actual) | Interventional | 2015-09-10 | Completed | ||
A Phase 1/1b Trial of MRTX849 in Combination With Palbociclib in Patients With Advanced Solid Tumors With KRAS G12C Mutation [NCT05178888] | Phase 1 | 11 participants (Actual) | Interventional | 2022-02-01 | Active, not recruiting | ||
A Phase III, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Inavolisib Plus Palbociclib and Fulvestrant Versus Placebo Plus Palbociclib and Fulvestrant in Patients With PIK3CA-Mutant, Hormone Receptor-Positive, He [NCT04191499] | Phase 2/Phase 3 | 325 participants (Anticipated) | Interventional | 2020-01-29 | Recruiting | ||
Multicentre, International Neoadjuvant Randomized Double-blind Trial Comparing Fulvestrant® to a Combination of Fulvestrant® and Palbociclib (CDK 4/6 Inhibitor) in Patients With Operable Luminal Breast Cancer Responding to Fulvestrant® [NCT03447132] | Phase 3 | 354 participants (Actual) | Interventional | 2017-12-20 | Completed | ||
A Pilot Study of IMMUNe mOdulation in Early Stage Estrogen Receptor Positive Breast Cancer Treated With neoADjuvant Avelumab, Palbociclib, and Endocrine Therapy: The ImmunoADAPT Study [NCT03573648] | Phase 2 | 33 participants (Actual) | Interventional | 2018-11-13 | Active, not recruiting | ||
A Phase 1, Open Label Study To Investigate The Effect Of Dose And Ethnicity On Palbociclib (PD-0332991) Pharmacokinetics In Japanese Healthy Volunteers [NCT02059330] | Phase 1 | 27 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
A Phase 1, Open-label, Single Dose, Parallel-group Study To Evaluate The Pharmacokinetics Of Palbociclib (Pd-0332991) In Subjects With Impaired Renal Function [NCT02085538] | Phase 1 | 31 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
A Phase Ib/II Study to Investigate the Safety, Tolerability, of APG-2575 as a Single Agent or in Combination With Systemic Anti-cancer Agents in Patients With ER Positive Breast Cancer or Advanced Solid Tumors. [NCT04946864] | Phase 1/Phase 2 | 65 participants (Anticipated) | Interventional | 2021-08-13 | Recruiting | ||
MATCH Treatment Subprotocol Z1B: Phase II Study of Palbociclib (PD-0332991) in Patients With Tumors With CCND1, 2, 3 Amplification [NCT04439201] | Phase 2 | 40 participants (Actual) | Interventional | 2016-05-31 | Active, not recruiting | ||
Phase II Single-arm Study of the Combination of Palbociclib and Cetuximab in KRAS/NRAS/BRAF Wild-type Metastatic Colorectal Cancer [NCT03446157] | Phase 2 | 24 participants (Actual) | Interventional | 2018-03-13 | Active, not recruiting | ||
A Phase 1, Open-Label, 6 Sequence, 3 Period, Crossover Study Of Palbociclib (PD-0332991) In Healthy Volunteers To Estimate The Relative Bioavailability Of 3 Palbociclib Formulations [NCT02083640] | Phase 1 | 30 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
A Phase II Randomized Study Evaluating the Biological and Clinical Effects of the Combination of Palbociclib With Letrozole as Neoadjuvant Therapy in Post-Menopausal Women With Estrogen-Receptor Positive Primary Breast Cancer [NCT02296801] | Phase 2 | 307 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
A Pilot Study Of Pd 0332991 In Patients With Previously Treated Mantle Cell Lymphoma [NCT00420056] | Phase 1 | 17 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
A Phase 1, Open-Label, Fixed-Sequence 2-Period Study To Investigate The Effect Of Multiple Doses Of Itraconazole On The Single Dose Pharmacokinetics of Palbociclib (PD-0332991) In Healthy Volunteers [NCT02131298] | Phase 1 | 12 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
Comparative Effectiveness of Palbociclib Plus Aromatase Inhibitor Versus Fulvestrant Alone as Initial Endocrine Therapy for HR+/HER2- Advanced Breast Cancer in Chinese Clinical Practice: a Real-world Study [NCT05000736] | 600 participants (Anticipated) | Observational | 2021-09-01 | Recruiting | |||
Phase II Open-label, Multicentre, Randomized Trial of Neoadjuvant Palbociclib in Combination With Hormonal Therapy and HER2 Blockade Versus Paclitaxel in Combination With HER2 Blockade for Postmenopausal Patients With Hormone Receptor Positive/HER2 Positi [NCT03644186] | Phase 2 | 144 participants (Actual) | Interventional | 2019-04-16 | Completed | ||
PHASE 1/2A DOSE ESCALATION, FINDING AND EXPANSION STUDY EVALUATING SAFETY, TOLERABILITY, PHARMACOKINETICS, PHARMACODYNAMICS AND ANTI TUMOR ACTIVITY OF PF-07104091 AS A SINGLE AGENT AND IN COMBINATION THERAPY [NCT04553133] | Phase 1/Phase 2 | 320 participants (Anticipated) | Interventional | 2020-09-16 | Recruiting | ||
Neoadjuvant Letrozole + Palbociclib in Patients With II-IIIB BC,HR+, HER2-, Phenotype and Pretreatment Recurrence Score(RS):18-25 or 26-100 by Oncotype DX Breast RS Assay.Analysis of RS and Pathological Changes at Surgery [NCT03819010] | Phase 2 | 66 participants (Actual) | Interventional | 2019-05-07 | Completed | ||
A Phase 1 Trial of PD0332991 and Paclitaxel in Patients With Rb-Expressing Advanced Breast Cancer [NCT01320592] | Phase 1 | 28 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
A Phase 1b Study of Palbociclib, Letrozole and Venetoclax in ER and BCL-2 Positive Locally Advanced or Metastatic Breast Cancer [NCT03900884] | Phase 1 | 36 participants (Anticipated) | Interventional | 2019-09-25 | Recruiting | ||
Asian, International, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase 3 Trial of Tamoxifen With or Without Palbociclib ± Goserelin in Women With Hormone Receptor-Positive, HER2-Negative Advanced or Metastatic Breast Cancer [NCT03423199] | Phase 3 | 180 participants (Anticipated) | Interventional | 2018-02-09 | Active, not recruiting | ||
"Neo-Adjuvant Treatment With the CDK4,6 Inhibitor Palbociclib in HER2-positive and ER-positive Breast Cancer: Effect on Ki67 and Apoptosis Before, During and After Treatment " [NCT02530424] | Phase 2 | 102 participants (Actual) | Interventional | 2015-05-31 | Completed | ||
Phase I Trial of Abexinostat Combined With Palbociclib and Fulvestrant in Patients With Antiestrogen Refractory ER+, HER2- Breast Cancer and Gynecological Metastatic Tumors [NCT04498520] | Phase 1 | 0 participants (Actual) | Interventional | 2021-03-31 | Withdrawn(stopped due to Funding) | ||
PHASE 1/2 STUDY TO EVALUATE PALBOCICLIB (IBRANCE®) IN COMBINATION WITH IRINOTECAN AND TEMOZOLOMIDE OR IN COMBINATION WITH TOPOTECAN AND CYCLOPHOSPHAMIDE IN PEDIATRIC PATIENTS WITH RECURRENT OR REFRACTORY SOLID TUMORS [NCT03709680] | Phase 2 | 184 participants (Anticipated) | Interventional | 2019-05-24 | Recruiting | ||
Targeted Agent and Profiling Utilization Registry (TAPUR) Study [NCT02693535] | Phase 2 | 3,791 participants (Anticipated) | Interventional | 2016-03-14 | Recruiting | ||
Phase Ib/IIa Study of Palbociclib in MLL-rearranged Acute Leukemias AMLSG 23-14/Palbo-AL-1 [NCT02310243] | Phase 1/Phase 2 | 50 participants (Anticipated) | Interventional | 2015-07-31 | Recruiting | ||
Los Tres Paso Trial: Step One - Neoadjuvant Palbociclib Monotherapy, Step Two - Concurrent Chemoradiation Therapy, and Step Three - Adjuvant Palbociclib Monotherapy in Patients With p16INK4a Negative, HPV-Unrelated Head and Neck Squamous Cell Carcinoma [NCT03389477] | Phase 2 | 26 participants (Actual) | Interventional | 2018-04-27 | Active, not recruiting | ||
Palbociclib in Combination With Fulvestrant or Tamoxifen as Treatment for Hormone Receptor Positive Metastatic Breast Cancer Previously Exposed to Inhibitors of the PI3K Pathway: A Phase II Study With Pharmacodynamics Markers [NCT02384239] | Phase 2 | 70 participants (Actual) | Interventional | 2015-10-19 | Completed | ||
AN OPEN-LABEL PHASE IB STUDY OF PALBOCICLIB (ORAL CDK 4/6 INHIBITOR) PLUS ABRAXANE (REGISTERED) (NAB-PACLITAXEL) IN PATIENTS WITH METASTATIC PANCREATIC DUCTAL ADENOCARCINOMA [NCT02501902] | Phase 1 | 76 participants (Actual) | Interventional | 2015-11-23 | Completed | ||
A Phase 1b/2a Study Of Palbociclib In Combination With Everolimus And Exemestane In Postmenopausal Women With Estrogen Receptor Positive and HER2 Negative Metastatic Breast Cancer [NCT02871791] | Phase 1/Phase 2 | 41 participants (Actual) | Interventional | 2016-08-24 | Completed | ||
Evaluation of Radiosurgery With Concurrent Cyclin-Dependent Kinase 4/6 Inhibitors in the Treatment of Brain Metastases [NCT04585724] | Phase 1 | 0 participants (Actual) | Interventional | 2020-06-12 | Withdrawn(stopped due to Closed due to low (0) accrual) | ||
A Phase II Study to Evaluate Efficacy, Safety and Tolerability of KN026 in Combination With Palbociclib and Fulvestrant in Patients With Locally Advanced HER2-positive Breast Cancer [NCT04778982] | 4 participants (Actual) | Observational | 2022-05-25 | Terminated(stopped due to Difficulty in completing enrollment within the planned time) | |||
A Biomarker Study of Palbociclib + Fulvestrant for Second, and Third Line of Postmenopausal Women With hr+/her2- Advanced Breast Cancer (PALPETBIO) [NCT03560856] | Phase 2 | 54 participants (Anticipated) | Interventional | 2018-06-27 | Not yet recruiting | ||
An Open Label Multicenter, Phase I-II Study With Tumor Molecular Pharmacodynamic (MPD) Evaluation and Pharmacokinetics of PD-0332991 in Patients Suffering Metastatic Melanoma With BRAFv600 Mutated and CDKN2A Loss and Expression of Rb and Treated by Vemura [NCT02202200] | Phase 1/Phase 2 | 40 participants (Anticipated) | Interventional | 2014-05-31 | Recruiting | ||
STUDY OF PALBOCICLIB IN COMBINATION WITH LETROZOLE AS TREATMENT OF POSTMENOPAUSAL WOMEN WITH HORMONE RECEPTOR POSITIVE, HER2-NEGATIVE ADVANCED BREAST CANCER FOR WHOM LETROZOLE THERAPY IS DEEMED APPROPRIATE [NCT02600923] | Phase 3 | 131 participants (Actual) | Interventional | 2016-04-15 | Completed | ||
Open-label, Randomized, Multicenter, International, Parallel Exploratory Phase II Study, Comparing 3 FEC-3 Docetaxel Chemotherapy to Letrozole + Palbociclib Combination as Neoadjuvant Treatment of Stage II-IIIA PAM 50 ROR-defined Low or Intermediate Risk [NCT02400567] | Phase 2 | 125 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
Treatment Patterns and Clinical Outcomes Among Patients Receiving Palbociclib Combinations for Hormone Receptor Positive (HR+)/Human Epidermal Growth Factor Receptor 2 Negative (HER2-) Advanced/Metastatic Breast Cancer in the Arabian Gulf Region Like Saud [NCT04916509] | 258 participants (Actual) | Observational | 2021-09-13 | Completed | |||
Retrospective, Multicenter, Observational Study to Evaluate Overall Survival in Japanese Patients With HR+/HER2- Advanced Breast Cancer Treated With Palbociclib Plus Letrozole [NCT04735367] | 42 participants (Anticipated) | Observational | 2021-02-03 | Active, not recruiting | |||
A Phase 1, Open-Label Fixed-Sequence 2-Period Crossover Study Of Palbociclib (pd-0332991) In Healthy Volunteers To Estimate The Effect Of Antacid Treatment On The Bioavailability Of A 125 Mg Single Dose Of Six Experimental Formulations Of Palbociclib Rela [NCT02311946] | Phase 1 | 60 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
Evaluation of the G8 Questionnaire and the Groningen Frailty Indicator to Predict Toxicities of CDK 4/6 Inhibitors in Older Breast Cancer Patients? [NCT05051956] | 140 participants (Anticipated) | Observational [Patient Registry] | 2021-10-01 | Not yet recruiting | |||
PALbociclib in Advanced Breast Cancer: Therapy INtegrating locorEgional Treatment and Palbociclib in de Novo, Treatment Naive, Stage IV ER+, HER2- Breast Cancer Patients [NCT03870919] | 200 participants (Actual) | Interventional | 2019-10-23 | Active, not recruiting | |||
A Phase II Study of Palbociclib, A CDK4/6 Inhibitor, in Patients With Metastatic Castration-Resistant Prostate Cancer [NCT02905318] | Phase 2 | 19 participants (Actual) | Interventional | 2017-07-04 | Active, not recruiting | ||
A Phase III Randomized, Double-Blind, Neoadjuvant Study of Hormonal Therapy Plus Palbociclib Versus Hormonal Therapy Plus Placebo in Women With Operable, Hormone Sensitive and HER2-Negative Primary Breast Cancer [NCT03969121] | Phase 3 | 141 participants (Actual) | Interventional | 2019-07-16 | Completed | ||
Biomarker and Tumor Cell Culture-Driven Pilot Trial for Treatment of Recurrent Glioblastoma [NCT05432518] | Early Phase 1 | 10 participants (Anticipated) | Interventional | 2023-06-27 | Recruiting | ||
A Phase III Open-label, Multicenter, Randomized Trial of Adjuvant Palbociclib in Combination With Endocrine Therapy Versus Endocrine Therapy Alone for Patients With Hormone Receptor Positive / HER2-negative Resected Isolated Locoregional Recurrence of Bre [NCT03820830] | Phase 3 | 400 participants (Anticipated) | Interventional | 2019-08-27 | Recruiting | ||
Neoadjuvant Treatment With Palbociclib and Exemestane Plus Trastuzumab and Pyrotinib in ER-positive, HER2-positive Breast Cancer (neoPEHP): an Exploratory, Open-label, Multi-center Phase 2 Study [NCT04858516] | Phase 2 | 57 participants (Anticipated) | Interventional | 2021-04-30 | Not yet recruiting | ||
Umbrella Protocol for Phase I/IIa Trials of Molecularly Matched Targeted Therapies Plus Radiotherapy in Patients With Newly Diagnosed Glioblastoma Without MGMT Promoter Methylation: NCT Neuro Master Match - N²M² (NOA-20) [NCT03158389] | Phase 1/Phase 2 | 228 participants (Actual) | Interventional | 2018-05-07 | Completed | ||
Optimal Dosing of Oral Anticancer Drugs in Older Adults With Cancer: a Randomized Pilot Study. [NCT05949424] | Phase 4 | 30 participants (Anticipated) | Interventional | 2024-05-31 | Not yet recruiting | ||
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524] | Phase 1 | 2 participants (Actual) | Interventional | 2020-04-01 | Active, not recruiting | ||
A Dutch National Study on Behalf of the CPCT to Facilitate Patient Access to Commercially Available, Targeted Anti-cancer Drugs to Determine the Potential Efficacy in Treatment of Advanced Cancers With a Known Molecular Profile [NCT02925234] | Phase 2 | 1,550 participants (Anticipated) | Interventional | 2016-08-31 | Recruiting | ||
Phase I/II Study of the CDK4/6 Inhibitor Palbociclib (PD-0332991) in Combination With the MEK Inhibitor Binimetinib (MEK162) for Patients With Advanced KRAS Mutant Non-Small Cell Lung Cancer [NCT03170206] | Phase 1/Phase 2 | 72 participants (Anticipated) | Interventional | 2017-05-31 | Recruiting | ||
Phase I Study of the CDK4/6 Inhibitor Palbociclib (PD-0332991) in Combination With the PI3K/mTOR Inhibitor Gedatolisib (PF-05212384) for Patients With Advanced Squamous Cell Lung, Pancreatic, Head & Neck and Other Solid Tumors [NCT03065062] | Phase 1 | 96 participants (Anticipated) | Interventional | 2017-02-28 | Recruiting | ||
Patterns of Treatment and Outcome of Palbociclib Plus Endocrine Therapy in Hormone Receptor-positive (HR+)/HER2 Receptor-negative (HER2-) Metastatic Breast Cancer (MBC): a Real World Multicentre Italian Study [NCT04524728] | 191 participants (Actual) | Observational [Patient Registry] | 2016-12-31 | Completed | |||
A Phase I Clinical, Pharmacokinetic, And Pharmacodynamic Evaluation Of 2 Schedules Of Oral PD 0332991, A Cyclin-Dependent Kinase Inhibitor, In Patients With Advanced Cancer [NCT00141297] | Phase 1 | 74 participants (Actual) | Interventional | 2004-09-30 | Completed | ||
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: Adaptive Clinical Treatment (ACT) [NCT05238831] | Early Phase 1 | 25 participants (Anticipated) | Interventional | 2023-12-01 | Not yet recruiting | ||
A Phase Ib/III, Open-label, Randomised Study of Capivasertib Plus CDK4/6 Inhibitors and Fulvestrant Versus CDK4/6 Inhibitors and Fulvestrant in Hormone Receptor-Positive and Human Epidermal Growth Factor Receptor 2-Negative Locally Advanced, Unresectable [NCT04862663] | Phase 3 | 850 participants (Anticipated) | Interventional | 2021-05-10 | Recruiting | ||
Phase IB/II Open-label Single Arm Study to Evaluate Safety and Efficacy of Tucatinib in Combination With Palbociclib and Letrozole in Subjects With Hormone Receptor Positive and HER2-positive Metastatic Breast Cancer [NCT03054363] | Phase 1/Phase 2 | 42 participants (Actual) | Interventional | 2017-11-27 | Completed | ||
Real-World Utilization of Palbociclib as 1L Treatment in Canadian HR+/HER2-women Breast Cancer Patients [NCT06003114] | 1 participants (Anticipated) | Observational | 2023-10-06 | Active, not recruiting | |||
REVERT- Breast Cancer: Phase 1b/2 Study of the Addition of STAT3 Inhibitor TTI-101 to Reverse Resistance to Palbociclib or Ribociclib Plus Aromatase Inhibitor or Fulvestrant Therapy for Metastatic Hormone Receptor-Positive and HER2-Negative Breast Cancer [NCT05384119] | Phase 1/Phase 2 | 53 participants (Anticipated) | Interventional | 2023-01-09 | Recruiting | ||
A Phase I Study of Palbociclib in Combination With Chemotherapy in Pediatric Patients With Relapsed or Refractory Acute Lymphoblastic Leukemia [NCT03515200] | Phase 1 | 12 participants (Actual) | Interventional | 2018-04-20 | Terminated(stopped due to Due to departure of PI from St. Jude) | ||
A Phase II Trial of Avelumab or Hydroxychloroquine With or Without Palbociclib to Eliminate Dormant Breast Cancer (PALAVY) [NCT04841148] | Phase 2 | 96 participants (Anticipated) | Interventional | 2021-06-01 | Recruiting | ||
PERFORM: An EPidEmiological, PRospective Cohort Study to Generate Real-world Evidence in Patients With HR+/HER2- Advanced Breast Cancer Treated in the First Line Setting as Per Current Standard Of Care With an EndocRine-based Palbociclib CoMbination Thera [NCT04767594] | 1,900 participants (Anticipated) | Observational | 2020-10-27 | Recruiting | |||
DEMOGRAPHICS, PATIENT CHARACTERISTICS, TREATMENT PATTERNS AND CLINICAL OUTCOMES OF PATIENTS TREATED WITH PALBOCICLIB IN A REAL LIFE SETTING IN ISRAEL [NCT04671615] | 559 participants (Actual) | Observational | 2020-12-06 | Completed | |||
A Phase II Trial Assessing the Tolerability of Palbociclib in Combination With Letrozole or Fulvestrant in Patients Aged 70 and Older With Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer [NCT03633331] | Phase 2 | 93 participants (Actual) | Interventional | 2018-08-15 | Active, not recruiting | ||
CDK4/6 Inhibitor Palbociclib Combined With Afatinib as Second-line Treatment for Advanced Squamous Carcinoma of the Esophagus or Gastroesophageal Junction Progressed on at Least First-line Chemotherapy: a Phase 2 Trial [NCT05865132] | Phase 2 | 30 participants (Anticipated) | Interventional | 2023-04-06 | Recruiting | ||
Multicenter, First-line Metastatic Open-label Prospective Phase II Trial Evaluating the Combination of Palbociclib (CDK 4/6 Inhibitor) and Hormone Therapy (Letrozole or Anastrozole) in Women With Luminal, HER2 Negative Advanced Breast Cancer: Evaluation o [NCT05190094] | Phase 2 | 80 participants (Anticipated) | Interventional | 2022-12-20 | Recruiting | ||
A Phase 1 Dose Escalation and Expansion Study of AZD9833 Alone or in Combination With Palbociclib or Everolimus in Chinese Patients With Oestrogen Receptor Positive (ER+), Human Epidermal Growth Factor Receptor 2 Negative (HER2-) Metastatic Breast Cancer [NCT04818632] | Phase 1 | 28 participants (Actual) | Interventional | 2021-11-12 | Completed | ||
The Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy [NCT04591431] | Phase 2 | 400 participants (Actual) | Interventional | 2020-10-07 | Active, not recruiting | ||
A Phase II Clinical Trail of the Cyclin Dependent Kinase (CDK)4/6 Inhibitor, PD0332991 in Previously Treated, Advanced NSCLC Patients With Wildtype Retinoblastoma Protein (RB) and Inactive Cyclin Dependent Kinase (CDK)N2a [NCT01291017] | Phase 2 | 19 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
A Phase I/II Multicenter Study of the Combination of AZD2014 and Palbociclib on a Background of Hormonal Therapy in Patients With Locally Advanced/Metastatic Estrogen Receptor Positive Breast Cancer Comprising a Safety, Pharmacokinetic and Preliminary Eff [NCT02599714] | Phase 1 | 54 participants (Actual) | Interventional | 2015-12-07 | Completed | ||
Palbociclib and Binimetinib in RAS-Mutant Cancers: A ComboMATCH Treatment Trial [NCT05554367] | Phase 2 | 199 participants (Anticipated) | Interventional | 2024-08-11 | Recruiting | ||
MULTICENTER, RANDOMIZED, DOUBLE-BLIND, PLACEBO-CONTROLLED, PHASE 3 TRIAL OF FULVESTRANT (FASLODEX (REGISTERED)). WITH OR WITHOUT PD-0332991 (PALBOCICLIB) +/- GOSERELIN IN WOMEN WITH HORMONE RECEPTOR-POSITIVE, HER2-NEGATIVE METASTATIC BREAST CANCER WHOSE D [NCT01942135] | Phase 3 | 521 participants (Actual) | Interventional | 2013-09-26 | Completed | ||
Phase II Trial of Palbociclib With Fulvestrant in Individuals With Hormone Receptor-Positive, HER2-Negative Metastatic Breast Cancer Who Have Progressed on Treatment With Palbociclib and an Aromatase Inhibitor [NCT02738866] | Phase 2 | 60 participants (Actual) | Interventional | 2016-10-25 | Active, not recruiting | ||
Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR): A Phase II Basket Trial [NCT03297606] | Phase 2 | 720 participants (Anticipated) | Interventional | 2018-03-23 | Recruiting | ||
Palbociclib After CDK and Endocrine Therapy (PACE): A Randomized Phase II Study of Fulvestrant, Palbociclib, and Avelumab for Endocrine Pre-treated ER+/HER2- Metastatic Breast Cancer [NCT03147287] | Phase 2 | 220 participants (Actual) | Interventional | 2017-09-05 | Active, not recruiting | ||
"Phase III Study Evaluating Palbociclib (PD-0332991), a Cyclin-Dependent Kinase (CDK) 4/6 Inhibitor in Patients With Hormone-receptor-positive, HER2-normal Primary Breast Cancer With High Relapse Risk After Neoadjuvant Chemotherapy PENELOPEB" [NCT01864746] | Phase 3 | 1,250 participants (Actual) | Interventional | 2013-10-30 | Completed | ||
A Phase II Single Arm Study of Palbociclib in Patients With Metastatic HER2-positive Breast Cancer With Brain Metastasis [NCT02774681] | Phase 2 | 12 participants (Actual) | Interventional | 2016-08-31 | Terminated(stopped due to Slow accrual) | ||
A Phase 1 Open-Label Study of the Safety and Efficacy of PD 0332991 (Palbociclib) in Combination With Lenalidomide and Dexamethasone in Patients With Relapsed or Refractory Multiple Myeloma [NCT02030483] | Phase 1 | 9 participants (Actual) | Interventional | 2014-02-28 | Terminated(stopped due to The company providing one of the study drugs withdrew its support due to low enrollment. Therefore, we had to close the study due to lack of funding.) | ||
Palbociclib and Cetuximab Versus Cetuximab Monotherapy for Patients With CDKN2A-altered, HPV-unrelated Head and Neck Squamous Cell Carcinoma Who Experienced Disease Progression on a PD-1/L1 Inhibitor: A Multicenter, Open-Label, Randomized Phase 3 Trial [NCT04966481] | Phase 3 | 81 participants (Anticipated) | Interventional | 2022-04-06 | Recruiting | ||
A Phase 2, International, Multicenter, Open-labeled, Randomized Trial of PAlbociclib and Fulvestrant vs. Standard Oral Capecitabine In Patients With Hormone Receptor (HR)+ / HER2- Advanced Breast Cancer and Documented Endocrine Resistance [NCT03322215] | Phase 2 | 42 participants (Actual) | Interventional | 2017-10-24 | Active, not recruiting | ||
A Dose-Escalation, Phase I/II, Open-Label, Three-Part Study of the MEK Inhibitor, Trametinib, Combined With the CDK4/6 Inhibitor, Palbociclib, To Investigate the Safety, Pharmacokinetics, Pharmacodynamics, and Anti-Cancer Activity in Subjects With Solid T [NCT02065063] | Phase 1 | 28 participants (Actual) | Interventional | 2014-04-22 | Completed | ||
SERENA-4: A Randomised, Multicentre, Double-Blind, Phase III Study of AZD9833 (an Oral SERD) Plus Palbociclib Versus Anastrozole Plus Palbociclib for the Treatment of Patients With Estrogen Receptor-Positive, HER2-Negative Advanced Breast Cancer Who Have [NCT04711252] | Phase 3 | 1,342 participants (Anticipated) | Interventional | 2021-01-28 | Recruiting | ||
Modular Phase 1B Hypothesis-Testing, Biomarker-Driven, Talazoparib Combination Trial (TalaCom) [NCT04693468] | Phase 1 | 111 participants (Anticipated) | Interventional | 2020-12-01 | Recruiting | ||
"Cyclin dEpendent Kinase in tRiple nEGatIVe brEast canceR - a Window of Opportunity Study" [NCT05067530] | Phase 2 | 126 participants (Anticipated) | Interventional | 2022-01-01 | Not yet recruiting | ||
A Phase II Study of Palbociclib for Previously Treated Cell Cycle Gene Alteration Positive Patients With Stage IV Squamous Cell Lung Cancer (Lung-Map Sub-Study) [NCT02785939] | Phase 2/Phase 3 | 53 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
A Phase1 Study at Stanford of Palbociclib in Combination With Chemotherapy in Pediatric Patients With Relapsed or Refractory Acute Lymphoblastic Leukemia (RELPALL2) [NCT04996160] | Phase 1 | 22 participants (Anticipated) | Interventional | 2021-07-09 | Recruiting | ||
Phase I Study of the Pan-ERBB Inhibitor Neratinib Given in Combination With Everolimus, Palbociclib, or Trametinib in Advanced Cancer Subjects With EGFR Mutation/Amplification, HER2 Mutation/Amplification, or HER3/4 Mutation or KRAS Mutation [NCT03065387] | Phase 1 | 93 participants (Actual) | Interventional | 2017-10-31 | Active, not recruiting | ||
A Phase 1, Open-label, 2-period, Fixed Sequence Study Of The Effect Of A Proton Pump Inhibitor On The Relative Bioavailability Of The Proposed Commercial Tablet Formulation Of Palbociclib In Healthy Volunteers [NCT03220191] | Phase 1 | 12 participants (Actual) | Interventional | 2017-07-21 | Completed | ||
A Phase 1, Open-Label, 3-Period Crossover Study Of The Effect Of An Antacid, A Proton Pump Inhibitor And An H2-Receptor Antagonist On Palbociclib (PD-0332991) Bioavailability Under Fed Conditions In Healthy Volunteers [NCT02097329] | Phase 1 | 27 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
Phase I/II Study of the CDK4/6 Inhibitor Palbociclib (PD-0332991) in Combination With the MEK Inhibitor PD-0325901 for Patients With KRAS Mutant Non-Small Cell Lung Cancer and Other Solid Tumors [NCT02022982] | Phase 1/Phase 2 | 139 participants (Anticipated) | Interventional | 2014-01-31 | Active, not recruiting | ||
A Multicenter, Open-label, Randomized, Phase 1/2 Study of Belzutifan in Combination With Palbociclib Versus Belzutifan Monotherapy in Participants With Advanced Renal Cell Carcinoma [NCT05468697] | Phase 1/Phase 2 | 180 participants (Anticipated) | Interventional | 2022-08-10 | Recruiting | ||
Avelumab, Palbociclib and Axitinib in in Treatment Naive Metastatic Clear Cell Renal Cell Carcinoma. [NCT05176288] | Phase 2 | 0 participants (Actual) | Interventional | 2024-05-31 | Withdrawn(stopped due to The overall protocol will be changed in a new amendment, which will be resubmitted under the new IND.) | ||
International,Multicenter,Randomized,Open-label, Phase II to Evaluate the Efficacy and Safety of Continuation of Palbociclib+2nd Line Endocrine Therapy in HR+/HER2- ABC Patients Who Had Clinical Benefit During 1st Line Palbociclib. [NCT03809988] | Phase 2 | 198 participants (Actual) | Interventional | 2019-04-05 | Completed | ||
Phase 1/2 Open-label Study Of The Safety And Efficacy Of Pd 0332991 In Combination With Bortezomib And Dexamethasone In Patients With Refractory Multiple Myeloma [NCT00555906] | Phase 2 | 53 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
A TREATMENT PROTOCOL FOR PARTICIPANTS CONTINUING FROM PFIZER-SPONSORED PALBOCICLIB CLINICAL STUDIES [NCT05226871] | Phase 2 | 35 participants (Anticipated) | Interventional | 2022-07-07 | Recruiting | ||
A Phase 1 Dose Escalation and Expansion Study to Evaluate Safety, Tolerability, Pharmacokinetic, Pharmacodynamic, and Anti-tumor Activity of PF-07248144 in Participants With Advanced or Metastatic Solid Tumors. [NCT04606446] | Phase 1 | 186 participants (Anticipated) | Interventional | 2020-11-16 | Recruiting | ||
A Phase III Randomized, Double-Blind, Placebo-Controlled, Multicenter Study Evaluating the Efficacy and Safety of GDC-9545 Combined With Palbociclib Compared With Letrozole Combined With Palbociclib in Patients With Estrogen Receptor-Positive, HER2-Negati [NCT04546009] | Phase 3 | 992 participants (Actual) | Interventional | 2020-10-09 | Active, not recruiting | ||
Phase I/II Safety and Efficacy Study of Autophagy Inhibition With Hydroxychloroquine to Augment the Antiproliferative and Biological Effects of Pre-Operative Palbociclib Plus Letrozole for Estrogen Receptor-Positive and HER2-Negative Breast Cancer [NCT03774472] | Phase 1/Phase 2 | 15 participants (Actual) | Interventional | 2018-08-20 | Active, not recruiting | ||
A Phase 1/2, Open Label, Dose Escalation, and Cohort Expansion Clinical Trial to Evaluate the Safety, Tolerability, and Pharmacokinetics of ARV-471 Alone and in Combination With Palbociclib (IBRANCE®) in Patients With Estrogen Receptor Positive/Human Epid [NCT04072952] | Phase 1/Phase 2 | 215 participants (Anticipated) | Interventional | 2019-08-05 | Recruiting | ||
Real-World Treatment Effectiveness of Palbociclib in Combination With an Aromatase Inhibitor as 1st Line Therapy in Metastatic Breast Cancer [NCT05361655] | 1 participants (Actual) | Observational | 2021-09-01 | Completed | |||
A Phase 1, Open-label, Fixed-sequence, 2-cohort, 2-period Study To Investigate The Effect Of Modafinil And Pioglitazone Given As Multiple Doses On Single Dose Pharmacokinetics Of Palbociclib (Pd-0332991) In Healthy Volunteers [NCT02222441] | Phase 1 | 14 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
A Phase 2 Study of Palbociclib in Progressive Brain Metastases Harboring Alterations in the CDK Pathway [NCT02896335] | Phase 2 | 30 participants (Anticipated) | Interventional | 2017-02-14 | Recruiting | ||
PALbociclib CoLlaborative Adjuvant Study: A Randomized Phase III Trial of Palbociclib With Standard Adjuvant Endocrine Therapy Versus Standard Adjuvant Endocrine Therapy Alone for Hormone Receptor Positive (HR+) / Human Epidermal Growth Factor Receptor 2 [NCT02513394] | Phase 3 | 5,796 participants (Actual) | Interventional | 2015-08-31 | Active, not recruiting | ||
Precise Targeted Therapy for Refractory HER2 Positive Advanced Breast Cancer Based on Genome Signature and Drug Sensitivity of PDO Model [NCT05429684] | Phase 3 | 120 participants (Anticipated) | Interventional | 2021-01-01 | Recruiting | ||
A Randomized, Open-label, Multi-center Phase IV Study Evaluating Palbociclib Plus Endocrine Treatment Versus a Chemotherapy-based Treatment Strategy in Patients With Hormone Receptor Positive / HER2 Negative Breast Cancer in a Real World Setting (GBG 93 - [NCT03355157] | Phase 4 | 150 participants (Anticipated) | Interventional | 2018-03-01 | Recruiting | ||
Phase II Study to Compare Fulvestrant (F) 500mg Plus Placebo vs F 500mg Plus Palbociclib as First Line Treatment for Postmenopausal Women With Hormone Receptor Positive Advanced Breast Cancer Sensitive to Endocrine Therapy. GEICAM/2014-12 [NCT02690480] | Phase 2 | 189 participants (Actual) | Interventional | 2016-02-17 | Active, not recruiting | ||
Single-arm Phase II Study of Palbociclib Plus Endocrine Therapy in Patients With High Risk ER-positive/HER2-negative T1-2N0-1 Early Breast Cancer Incorporating GenesWell™ BCT [NCT04247633] | Phase 2 | 578 participants (Anticipated) | Interventional | 2020-02-11 | Recruiting | ||
PErsonalized TREatment of High-risk MAmmary Cancer - the PETREMAC Trial [NCT02624973] | Phase 2 | 200 participants (Actual) | Interventional | 2016-04-15 | Active, not recruiting | ||
A Phase II Study of Palbociclib Plus Fulvestrant for Pretreated Patients With ER+/HER2- Metastatic Breast Cancer [NCT02536742] | Phase 2 | 124 participants (Actual) | Interventional | 2016-08-30 | Active, not recruiting | ||
A Phase 1 Dose Escalation and Expansion Study of AZD9833 Alone or in Combination in Women With ER-positive, HER2-negative Advanced Breast Cancer (SERENA-1) [NCT03616587] | Phase 1 | 386 participants (Anticipated) | Interventional | 2018-10-11 | Recruiting | ||
A Single Arm Phase II Study to Evaluate Efficacy of T-DM1 With Palbociclib in the Treatment of Patients With Metastatic HER2 Positive Breast Cancer [NCT03530696] | Phase 2 | 54 participants (Actual) | Interventional | 2018-12-06 | Completed | ||
A Multicenter, Open-label, Phase I Clinical Study to Evaluate the Safety, Pharmacokinetics, and Antitumor Efficacy of SIM0270 Alone or in Combination in Subjects With ER-positive, HER-2 Negative Locally Advanced or Metastatic Breast Cancer [NCT05293964] | Phase 1 | 210 participants (Anticipated) | Interventional | 2022-05-18 | Recruiting | ||
A Randomized, Open Label, Phase III Trial to Evaluate the Efficacy and Safety of Palbociclib + Anti-HER2 Therapy + Endocrine Therapy vs. Anti-HER2 Therapy + Endocrine Therapy After Induction Treatment for Hormone Receptor Positive (HR+)/HER2-Positive Meta [NCT02947685] | Phase 3 | 496 participants (Anticipated) | Interventional | 2017-06-21 | Active, not recruiting | ||
A Phase II, Open-Label, Multicenter, Platform Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors [NCT04931342] | Phase 2 | 550 participants (Anticipated) | Interventional | 2021-10-07 | Recruiting | ||
Perioperative Analysis of Binimetinib and Palbociclib in RAS-Driven Tumors [NCT04870034] | Early Phase 1 | 0 participants (Actual) | Interventional | 2024-01-15 | Withdrawn(stopped due to Issues recruiting) | ||
PAveMenT: Phase Ib Study of Palbociclib and Avelumab in Metastatic AR+ Triple Negative Breast Cancer [NCT04360941] | Phase 1 | 45 participants (Anticipated) | Interventional | 2020-08-11 | Recruiting | ||
A Phase 2 Pilot Feasibility Study of Palbociclib in Combination With Adjuvant Endocrine Therapy for Hormone Receptor Positive Invasive Breast Carcinoma [NCT02040857] | Phase 2 | 162 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
Randomized, Open Label, Multicentric Phase III Trial to Evaluate the Safety and Efficacy of Palbociclib in Combination With HT Driven by ctDNA ESR1 Mutation Monitoring in ER+, HER2-negative Metastatic Breast Cancer Patients [NCT03079011] | Phase 3 | 1,017 participants (Actual) | Interventional | 2017-03-22 | Active, not recruiting | ||
A Phase 1/2 Open Label, Multicenter Study to Assess the Safety, Tolerability, Pharmacokinetics, and Anti-Tumor Activity of ZN-c5 Alone and in Combination With Palbociclib in Subjects With Estrogen-Receptor Positive, Human Epidermal Growth Factor Receptor- [NCT03560531] | Phase 1/Phase 2 | 181 participants (Actual) | Interventional | 2018-12-08 | Completed | ||
Palbociclib, Trastuzumab, Pyrotinib and Fulvestrant Treatment in Patients With Brain Metastasis From ER/PR Positive, HER-2 Positive Breast Cancer: A Multi-center, Prospective Study in China [NCT04334330] | Phase 2 | 34 participants (Anticipated) | Interventional | 2020-12-04 | Recruiting | ||
AN EXPANDED ACCESS STUDY OF PALBOCICLIB IN COMBINATION WITH LETROZOLE AS TREATMENT OF POST-MENOPAUSAL WOMEN WITH HORMONE RECEPTOR POSITIVE, HER2 NEGATIVE ADVANCED BREAST CANCER FOR WHOM LETROZOLE THERAPY IS DEEMED APPROPRIATE [NCT02142868] | 0 participants | Expanded Access | No longer available | ||||
PRECYCLE: Multicenter, Randomized Phase IV Intergroup Trial to Evaluate the Impact of eHealth-based Patient Reported Outcome (PRO) Assessment on Quality of Life in Patients With Hormone Receptor Positive, HER2 Negative Locally Advanced or Metastatic Breas [NCT03220178] | Phase 4 | 532 participants (Actual) | Interventional | 2017-07-24 | Terminated(stopped due to Due to COVID-19 pandemic, study cannot be finished in planned timeframe.) | ||
Retrospective Observational Analysis of Palbociclib Treatment in Patients With Advanced Breast Cancer Within a Compassionate Use Programme [NCT04109261] | 237 participants (Actual) | Observational | 2018-09-18 | Completed | |||
PREDIX Luminal B - Neoadjuvant Response-guided Treatment of ER Positive Tumors With High Proliferation or Low Proliferation With Metastatic Nodes. Part of a Platform of Translational Phase II Trials Based on Molecular Subtypes [NCT02603679] | Phase 2 | 181 participants (Actual) | Interventional | 2015-02-28 | Active, not recruiting | ||
A Phase II Randomized Study of Palbociclib in Combination With Exemestane Plus GnRH Versus Capecitabine in Premenopausal Women With Hormone Receptor-Positive Metastatic Breast Cancer [NCT02592746] | Phase 2 | 182 participants (Anticipated) | Interventional | 2016-06-30 | Active, not recruiting | ||
Randomized Phase II Study of Elacestrant vs Elacestrant Plus a CDK4/6 Inhibitor (Palbociclib, Abemaciclib, or Ribociclib) in Patients With ER+/HER2- Advanced or Metastatic Breast Cancer With Prior Exposure to a CKD4/6 Inhibitor [NCT06062498] | Phase 2 | 174 participants (Anticipated) | Interventional | 2023-09-30 | Not yet recruiting | ||
REAL-WORLD TUMOR RESPONSE OF PALBOCICLIB IN COMBINATION WITH AN AROMATASE INHIBITOR AS FIRST-LINE THERAPY IN PRE/PERIMENOPAUSAL WOMEN WITH METASTATIC BREAST CANCER [NCT05012644] | 197 participants (Actual) | Observational | 2021-02-17 | Completed | |||
An Assessment of the Biological and Clinical Effects of Palbociclib (PD 0332991) With Ovarian Suppression and Letrozole in the Neoadjuvant Treatment of Patients With Premenopausal Estrogen-Receptor Positive/HER2-Negative Primary Breast Cancer [NCT03628066] | Phase 2 | 24 participants (Actual) | Interventional | 2018-10-22 | Completed | ||
CIMER: Combined Immunotherapies in Metastatic ER+ Breast Cancer [NCT04220476] | Phase 2 | 0 participants (Actual) | Interventional | 2020-03-04 | Withdrawn(stopped due to Initiating a new study with revised Statistics.) | ||
A PHASE 3, RANDOMIZED, OPEN-LABEL, MULTICENTER STUDY OF ARV-471(PF-07850327) PLUS PALBOCICLIB VERSUS LETROZOLE PLUS PALBOCICLIB FOR THE TREATMENT OF PARTICIPANTS WITH ESTROGEN RECEPTOR-POSITIVE, HER2-NEGATIVE BREAST CANCER WHO HAVE NOT RECEIVED ANY PRIOR [NCT05909397] | Phase 3 | 1,180 participants (Anticipated) | Interventional | 2023-08-09 | Recruiting | ||
Randomised Phase II Study of Induction Fulvestrant and CDK4/6 Inhibition With the Addition of Ipatasertib in Metastatic ER+/HER2- Breast Cancer Patients Without ctDNA Suppression [NCT04920708] | Phase 2 | 324 participants (Anticipated) | Interventional | 2022-12-28 | Recruiting | ||
A Phase Ib/II Study Confirmed Inhibition of Autophagy Synergizes Anti-tumor Effect of High Dose CDK4/6i With Manageable Safety in HR+HER2-breast Cancer Patients [NCT05953350] | Phase 1/Phase 2 | 29 participants (Anticipated) | Interventional | 2023-06-12 | Recruiting | ||
An Open-Label, Phase Ia/Ib/IIa Study of GDC-0810 Single Agent or in Combination With Palbociclib and/or an LHRH Agonist in Women With Locally Advanced or Metastatic Estrogen Receptor Positive Breast Cancer [NCT01823835] | Phase 1/Phase 2 | 152 participants (Actual) | Interventional | 2014-12-29 | Terminated(stopped due to The Sponsor decided to halt the development of GDC-0810, but not due to any safety concerns.) | ||
Pilot Trial of Anastrozole and Palbociclib as First-Line Therapy and as Maintenance Therapy After First Line Chemotherapy in Hormone Receptor Positive, HER2-Negative Postmenopausal Metastatic Breast Cancer [NCT02942355] | Phase 2 | 40 participants (Anticipated) | Interventional | 2016-12-07 | Active, not recruiting | ||
A Retrospective Study of Prediction of 18F-FES-PET/CT Parameters on the Outcome of Palbociclib Combined With Endocrine Therapy in Patients With HR+ and HER2-metastatic Breast Cancer [NCT04992156] | 50 participants (Actual) | Observational | 2017-03-15 | Completed | |||
A Phase II Clinical Trial Assessing the Safety of an Alternative Dosing Schedule of Palbociclib in Metastatic Hormone Receptor Positive Breast Cancer [NCT03007979] | Phase 2 | 55 participants (Actual) | Interventional | 2017-06-15 | Completed | ||
A Phase I Trial of Palbociclib and Bosutinib With Fulvestrant in Patients With Metastatic Hormone Receptor Positive and HER2 Negative (HR+ HER2-) Breast Cancer Refractory to an Aromatase Inhibitor and a CDK4/6 Inhibitor (ASPIRE - WI231696) [NCT03854903] | Phase 1 | 19 participants (Actual) | Interventional | 2019-04-01 | Active, not recruiting | ||
Efficacy, Tolerability, and Safety of Palbociclib Combined With an Aromatase Inhibitor in Hormone Receptor-positive/Human Epidermal Growth Factor Receptor 2-negative Locally Advanced Breast Cancer [NCT04047758] | Phase 3 | 420 participants (Anticipated) | Interventional | 2019-09-01 | Recruiting | ||
Observational Cohort Study of Patients With Hormone Receptor-positive Metastatic Breast Cancer Treated With Palbociclib (Ibrance(Registered)) as Part of the United Kingdom Ibrance (Registered) Patient Program (IPP); the Real Outcomes Ibrance (Registered) [NCT03921866] | 191 participants (Actual) | Observational | 2019-03-01 | Completed | |||
Phase 2,Open-label,Multicenter,Randomized Study of PD0332991 (Oral CDK4/6 Inhibitor) Monotherapy and in Combination With the HT to Which the pt Has Progressed in the Previous Line for ER+,Her2- Post-menopausal Advanced Breast Cancer Pts [NCT02549430] | Phase 2 | 115 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
Randomized Short-term Pre-surgical Study to Assess the Effects of PD 0332991 in Early Breast Cancer Patients [NCT02008734] | Phase 2 | 132 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
PREDIX Luminal A - Neoadjuvant Response-guided Treatment of Slowly Proliferating Hormone Receptor Positive Tumors. Part of a Platform of Translational Phase II Trials Based on Molecular Subtypes [NCT02592083] | Phase 2 | 10 participants (Actual) | Interventional | 2015-10-31 | Active, not recruiting | ||
PHASE 1/2, OPEN-LABEL, RANDOMIZED STUDY OF THE SAFETY, EFFICACY, AND PHARMACOKINETICS OF LETROZOLE PLUS PD 0332991 (ORAL CDK 4/6 INHIBITOR) AND LETROZOLE SINGLE AGENT FOR THE FIRST-LINE TREATMENT OF ER POSITIVE, HER2 NEGATIVE ADVANCED BREAST CANCER IN POS [NCT00721409] | Phase 2 | 177 participants (Actual) | Interventional | 2008-09-15 | Completed | ||
National Lung Matrix Trial: Multi-drug, Genetic Marker-directed, Non-comparative, Multi-centre, Multi-arm Phase II Trial in Non-small Cell Lung Cancer [NCT02664935] | Phase 2 | 423 participants (Actual) | Interventional | 2015-05-31 | Active, not recruiting | ||
A Phase 1, Open-Label 4 Sequence 4 Period Crossover Study Of Palbociclib (PD-0332991) In Healthy Volunteers To Estimate The Effect Of Food On The Bioavailability Of Palbociclib [NCT01904747] | Phase 1 | 28 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
A Phase 1, Open-Label 3 Sequence 3 Period Crossover Study Of Palbociclib (PD-0332991) In Healthy Volunteers To Establish The Bioequivalence Of The Phase 1/2 And Phase 3 Formulation To Palbociclib ICH Formulation Under Fasted Conditions [NCT01906125] | Phase 1 | 73 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
A Phase 1, Open-Label Fixed-Sequence 2-Period Crossover Study Of Palbociclib In Healthy Subjects To Investigate The Potential Effect Of Antacid Treatment On The Pharmacokinetics Of A Single Oral Dose Administered Under Fasted Conditions [NCT01918176] | Phase 1 | 26 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
Unveiling Prognosis Cancer-Associated Thromboembolism Biomarkers and Their Related Polymorphisms: Exploring Their Involvement With Immune Circulating Cells and Therapeutic Reversibility [NCT06065592] | Phase 1 | 500 participants (Anticipated) | Interventional | 2019-02-01 | Recruiting | ||
A Phase Ib/III Study of Ipatasertib Plus Palbociclib and Fulvestrant Versus Placebo Plus Palbociclib and Fulvestrant in Hormone Receptor Positive and HER2 Negative Locally Advanced Unresectable or Metastatic Breast Cancer [NCT04060862] | Phase 3 | 20 participants (Actual) | Interventional | 2019-11-15 | Completed | ||
Harnessing Olaparib, Palbociclib and Endocrine Therapy: A Phase I/II Trial of Olaparib, Palbociclib and Fulvestrant in Patients With BRCA Mutation-associated, Hormone Receptor-positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Metastatic B [NCT03685331] | Phase 1 | 54 participants (Anticipated) | Interventional | 2020-10-15 | Active, not recruiting | ||
A Phase 1, Open-Label Fixed-Sequence 2-Period Study To Investigate The Effect Of Multiple Doses Of Rifampin On Palbociclib (PD-0332991) Pharmacokinetics In Healthy Volunteers [NCT01953731] | Phase 1 | 15 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
A Phase 1/2, First-in-Human Study to Assess the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, MTD/RP2D, and Antitumor Activity of ARTS-021 as a Single Agent and in Combination Therapy in Patients With Solid Tumors [NCT05867251] | Phase 1/Phase 2 | 192 participants (Anticipated) | Interventional | 2023-08-30 | Recruiting | ||
A Phase 1 Open-Label Fixed-Sequence Two-Period Crossover Study Of The Effect Of Multiple Doses Of Tamoxifen On PD-0332991 Pharmacokinetics In Healthy Male Volunteers [NCT01821066] | Phase 1 | 25 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
A Phase Ib/II, Open-Label, Multicenter, Randomized Umbrella Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Breast Cancer (MORPHEUS- BREAST CANCER) [NCT04802759] | Phase 1/Phase 2 | 510 participants (Anticipated) | Interventional | 2021-06-20 | Recruiting | ||
Randomized Phase II Study Comparing Two Different Schedules of Palbociclib Plus Second Line Endocrine Therapy in Women With Estrogen Receptor Positive, HER2 Negative Advanced/Metastatic Breast Cancer [NCT02630693] | Phase 2 | 180 participants (Actual) | Interventional | 2016-04-08 | Completed | ||
A Phase II Trial of Neoadjuvant PD 0332991, a Cyclin-Dependent Kinase (Cdk) 4/6 Inhibitor, in Combination With Anastrozole in Women With Clinical Stage 2 or 3 Estrogen Receptor Positive and HER2 Negative Breast Cancer [NCT01723774] | Phase 2 | 84 participants (Actual) | Interventional | 2013-04-10 | Active, not recruiting | ||
A Phase II Study of PD-0332991 in Adult Patients With Advanced Hepatocellular Carcinoma [NCT01356628] | Phase 2 | 23 participants (Actual) | Interventional | 2011-05-25 | Active, not recruiting | ||
Precision Treatment of Locoregionally Advanced Nasopharyngeal Carcinoma Based on Molecular Immune Subtyping: an Umbrella Trial [NCT04605562] | Phase 2 | 206 participants (Anticipated) | Interventional | 2022-06-30 | Not yet recruiting | ||
Phase 3, Open-Label, Randomized, Study Comparing Gedatolisib Combined With Fulvestrant & With or Without Palbociclib to Standard-of-Care Therapies in Patients With HR-Positive, HER2-Negative Advanced Breast Cancer Previously Treated With a CDK4/6 Inhibito [NCT05501886] | Phase 3 | 701 participants (Anticipated) | Interventional | 2022-09-30 | Recruiting | ||
A Phase 1, Open-label 6 Sequence 3 Period Crossover Study of Palbociclib (PD- 0332991) in Healthy Volunteers to Estimate the Relative Bioavailability of Palbociclib Formulations [NCT02041273] | Phase 1 | 36 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
An Open-Label Multicenter Phase 1b Study of H3B-6545 in Combination With Palbociclib in Women With Advanced or Metastatic Estrogen Receptor-Positive HER2-Negative Breast Cancer [NCT04288089] | Phase 1 | 36 participants (Anticipated) | Interventional | 2020-04-01 | Active, not recruiting | ||
A Randomized Phase II Trial Of Circulating Tumor DNA-Guided Second Line Adjuvant Therapy For High Residual Risk, Stage II-III, Hormone Receptor Positive, HER2 Negative Breast Cancer [NCT04567420] | Phase 2 | 100 participants (Anticipated) | Interventional | 2021-02-09 | Recruiting | ||
Phase III Study of Palbociclib in Combination With Exemestane or Fulvestrant vs. Chemotherapy (Capecitabine) in Hormonal Receptor Positive/HER2 Negative Metastatic Breast Cancer Patients With Resistance to Aromatase Inhibitors [NCT02028507] | Phase 3 | 693 participants (Actual) | Interventional | 2014-03-13 | Completed | ||
A Phase II Clinical Study on Efficacy of Palbociclib in Advanced Acral Melanoma With Cell Cycle Gene Aberrations [NCT03454919] | Phase 2 | 60 participants (Anticipated) | Interventional | 2018-03-30 | Not yet recruiting | ||
Non-Interventional, National Study Of Real-World Evidence In Estrogen Receptor Positive, Her2 Negative Metastatic Breast Cancer Patients Treated With Palbociclib During a 2.5 Years Follow-Up Period [NCT05135104] | 650 participants (Anticipated) | Observational | 2021-12-15 | Recruiting | |||
Phase IV Multi-arm Study of CDK4/6 Pharmacokinetics in Healthy Volunteers With Known CYP3A4*22 Genotype [NCT05691400] | Phase 4 | 45 participants (Anticipated) | Interventional | 2023-12-31 | Not yet recruiting | ||
A Phase III, Double-blind, Randomised Study to Assess Switching to AZD9833 (a Next Generation, Oral SERD) + CDK4/6 Inhibitor vs Continuing Aromatase Inhibitor (Letrozole or Anastrozole)+ CDK4/6 Inhibitor in HR+/HER2-MBC Patients With Detectable ESR1Mutati [NCT04964934] | Phase 3 | 300 participants (Anticipated) | Interventional | 2021-06-30 | Recruiting | ||
Palbociclib Plus Fulvestrant in Women With Hormone Receptor Positive and Human Epidermal Growth Factor Receptor Type 2 Negative Locally Advanced or Metastatic Breast Cancer Previously Treated With a CDK4/6 Inhibitor in Combination With Hormonal Therapy: a [NCT04318223] | Phase 2 | 168 participants (Anticipated) | Interventional | 2019-07-16 | Recruiting | ||
A Phase II Trial to Assess the Activity and Safety of Palbociclib in Patients With Well and Moderately Differentiated Metastatic Pancreatic Neuroendocrine Tumors (pNET) [NCT02806648] | Phase 2 | 21 participants (Actual) | Interventional | 2015-05-31 | Completed | ||
A Phase 1 Study Of Palbociclib (IND#141416), A CDK 4/6 Inhibitor, In Combination With Chemotherapy In Children With Relapsed Acute Lymphoblastic Leukemia (ALL) Or Lymphoblastic Lymphoma (LL) [NCT03792256] | Phase 1 | 15 participants (Anticipated) | Interventional | 2019-04-11 | Active, not recruiting | ||
An Open, Multicenter Study for the Predicted Biomarkers of CDK4/6 Inhibitors (Palbociclib) in ER-positive Metastasis Breast Cancer [NCT04289974] | 100 participants (Anticipated) | Observational | 2019-02-14 | Recruiting | |||
A Phase II Trial of Palbociclib in Combination With Trastuzumab and Endocrine Therapy in Patients With Previously-treated Locally Advanced or Metastatic HER2-positive Breast Cancer (PATRICIA II) [NCT02448420] | Phase 2 | 102 participants (Anticipated) | Interventional | 2015-07-31 | Active, not recruiting | ||
Palbociclib + Letrozole Versus Epirubicin + Cyclophosphamide and Sequential Docetaxel as Neoadjuvant Chemotherapy for Postmenopausal Estrogen Receptor-positive Breast Cancer: a Prospective Randomized Controlled Double-blind Phase IV Trial [NCT04137640] | Phase 4 | 152 participants (Anticipated) | Interventional | 2021-07-19 | Not yet recruiting | ||
Phase I/II Trial of the Addition of PD 0332991 to Cetuximab in Patients With Incurable SCCHN [NCT02101034] | Phase 1/Phase 2 | 96 participants (Actual) | Interventional | 2014-06-17 | Completed | ||
An International, Non-controlled Phase II Trial to Identify the Molecular Mechanisms of Resistance and Sensitivity to Palbociclib Re-challenge Upon Progression to a Palbociclib Combination in ER-positive Metastatic Breast Cancer Patients [NCT03184090] | Phase 2 | 33 participants (Actual) | Interventional | 2017-06-28 | Completed | ||
Phase IB Clinical Trial of Palbociclib and Binimetinib in Advanced Triple Negative Breast Cancer With Hyperactivation of ERK and/or CDK4/6 [NCT04494958] | Phase 1/Phase 2 | 24 participants (Actual) | Interventional | 2020-11-18 | Completed | ||
Rogaratinib, Palbociclib and Fulvestrant in Advanced Hormone Receptor Positive, FGFR1/2/3-positive Breast Cancer: Phase I Clinical Trial Plus an Expansion Cohort [NCT04483505] | Phase 1 | 9 participants (Actual) | Interventional | 2020-11-25 | Completed | ||
A Real-world Analysis of Concomitant Medication Use Among Metastatic Breast Cancer Patients Treated With CDK4/6 Inhibitors [NCT05141240] | 4,650 participants (Actual) | Observational | 2020-04-15 | Completed | |||
A Phase II Study of Ovarian Function Suppression And ExemesTane With or Without PalbocIclib in PreMenopausal Women With ER Positive / HER-2 Negative MetAstatic Breast Cancer [NCT02917005] | Phase 2 | 160 participants (Anticipated) | Interventional | 2019-05-07 | Recruiting | ||
A Multicenter, Phase I/II Trial of Anastrozole, Palbociclib, Trastuzumab and Pertuzumab in HR-positive, HER2-positive Metastatic Breast Cancer [NCT03304080] | Phase 1/Phase 2 | 44 participants (Actual) | Interventional | 2017-12-20 | Active, not recruiting | ||
A Phase II Study Of PD0332991 (Palbociclib) in Patients With Advanced or Metastatic Liposarcoma [NCT01209598] | Phase 2 | 90 participants (Actual) | Interventional | 2010-09-23 | Completed | ||
A Phase II Neoadjuvant Study of Palbociclib in Combination With Letrozole and Trastuzumab as Neoadjuvant Treatment of Stage II-III ER+ HER2+ Breast Cancer (PALTAN) [NCT02907918] | Phase 2 | 26 participants (Actual) | Interventional | 2017-06-30 | Terminated(stopped due to Futility) | ||
A Phase 1, Open-label, Single Dose, Parallel-cohort Study To Evaluate The Pharmacokinetics Of Palbociclib (Pd-0332991) In Subjects With Impaired Hepatic Function [NCT02334800] | Phase 1 | 28 participants (Actual) | Interventional | 2015-03-31 | Completed | ||
Levels of Circulating Tumor DNA as a Predictive Marker for Early Switch in Treatment for Patients With Metastatic (Stage IV) Breast Cancer: A Phase 2 Randomized, Open-Label Study [NCT05826964] | Phase 2 | 500 participants (Anticipated) | Interventional | 2023-06-12 | Recruiting | ||
BOOG 2017-03: Endocrine Therapy Plus CDK 4/6 Inhibition in First- or Second-line for Hormone Receptor Positive Advanced Breast Cancer - the SONIA Study [NCT03425838] | Phase 3 | 1,050 participants (Actual) | Interventional | 2017-11-09 | Active, not recruiting | ||
Treatment Patterns and Clinical Outcomes Among Indian Patients Receiving Palbociclib Combinations for HR+/HER2- Advanced/Metastatic Breast Cancer in Real World Settings [NCT05584644] | 150 participants (Actual) | Observational | 2021-05-24 | Completed | |||
Molecular Analysis for Combination Therapy Choice (ComboMATCH) [NCT05564377] | Phase 2 | 2,900 participants (Anticipated) | Interventional | 2023-04-07 | Recruiting | ||
Phase I Study of Palbociclib Alone and in Combination in Patients With Relapsed and Refractory Leukemias [NCT03132454] | Phase 1 | 54 participants (Anticipated) | Interventional | 2017-07-25 | Recruiting | ||
Open-label, Multi-center, sINGlE Arm Clinical Study to Evaluate Efficacy/QoL in Women With HR+, HER2-, Regionally Recurrent or Metastatic Breast Cancer Receiving Palbociclib With an AI or Fulvestrant After Prior Endocrine Therapy [NCT02894398] | Phase 2 | 388 participants (Actual) | Interventional | 2016-09-06 | Completed | ||
Palbociclib Plus Letrozole Treatment After Progression to Second Line Chemotherapy for Women With ER/PR-positive Ovarian Cancer. [NCT03936270] | Phase 2 | 43 participants (Actual) | Interventional | 2020-01-27 | Active, not recruiting | ||
Phase II Trial of the Cyclin-Dependent Kinase Inhibitor PD 0332991 in Patients With Cancer [NCT01037790] | Phase 2 | 304 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
A Phase I Trial of Ulixertinib (BVD-523) in Combination With Palbociclib in Patients With Advanced Solid Tumors With Expansion Cohort in Previously Treated Metastatic Pancreatic Cancer and Metastatic RAS-mutant and NF1-mutant (no Concurrent BRAFV600 Mutat [NCT03454035] | Phase 1 | 45 participants (Anticipated) | Interventional | 2018-01-30 | Recruiting | ||
Phase Ib Trial Evaluating the Combination of CDK4 Inhibitor With Immunotherapy in Patients With Undifferentiated Pleomorphic Sarcoma (UPS) [NCT06113809] | Phase 1 | 8 participants (Anticipated) | Interventional | 2024-01-31 | Not yet recruiting | ||
CDK4/6 Inhibition in Locally Advanced/Metastatic Chordoma (NCT-PMO-1601) [NCT03110744] | Phase 2 | 43 participants (Actual) | Interventional | 2017-12-15 | Completed | ||
Treatment of Metastatic Breast Cancer With Fulvestrant Plus Palbociclib or Tamoxifen Plus Palbociclib: A Randomized Pilot Trial With ESR1 Mutation Tested in Circulating Tumor DNA. [NCT02913430] | Early Phase 1 | 7 participants (Actual) | Interventional | 2018-04-24 | Active, not recruiting | ||
A Pilot Study of Personalized Biomarker-based Treatment Strategy or Immunotherapy in Patients With Recurrent/Metastatic Squamous Cell Carcinoma of the Head and Neck [NCT03088059] | Phase 2 | 340 participants (Anticipated) | Interventional | 2017-11-16 | Active, not recruiting | ||
Phase I/II Trial of Palbociclib in Combination With Bicalutamide for the Treatment of AR(+) Metastatic Breast Cancer (MBC) [NCT02605486] | Phase 1/Phase 2 | 46 participants (Actual) | Interventional | 2015-11-11 | Active, not recruiting | ||
A Phase I Study of the CDK4/6 Inhibitor PD-0332991, 5-Fluorouracil, and Oxaliplatin in Patients With Advanced Solid Tumor Malignancies [NCT01522989] | Phase 1 | 37 participants (Actual) | Interventional | 2011-12-31 | Active, not recruiting | ||
A Open Label Phase II Study of the Efficacy and Safety of PD0332991 a Selective Inhibitor of the Cyclin Dependent Kinases 4 and 6 in Patients With Recurrent Ovarian Cancer Demonstrating Rb-proficiency and Low p16 Expression [NCT01536743] | Phase 2 | 26 participants (Actual) | Interventional | 2011-12-15 | Completed | ||
Early Identification of Patients Who Benefit From Palbociclib in Addition to Letrozole [NCT02806050] | Phase 2 | 30 participants (Actual) | Interventional | 2016-09-16 | Completed | ||
A Phase II Study of Adjuvant PALbociclib as an Alternative to CHemotherapy in Elderly patientS With High-risk ER+/HER2- Early Breast Cancer [NCT03609047] | Phase 2 | 366 participants (Anticipated) | Interventional | 2019-06-14 | Active, not recruiting | ||
A Randomized, Open-label, Parallel-group Study Comparing the Immune Modulation Effect of Ribociclib, Palbociclib, and Abemaciclib in Early ER+/HER2- Breast Cancer [NCT05766410] | Phase 2 | 60 participants (Anticipated) | Interventional | 2022-09-16 | Recruiting | ||
A Phase 1B Study to Evaluate the Safety, Tolerability and Preliminary Efficacy of the Combination of Encorafenib, Binimetinib and Palbociclib in Patients With BRAF-mutant Metastatic Melanoma (The CELEBRATE Study) [NCT04720768] | Phase 1/Phase 2 | 78 participants (Anticipated) | Interventional | 2020-06-04 | Recruiting | ||
Phase I/II Trial of CPX-351 + Palbociclib in Patients With Acute Myeloid Leukemia [NCT03844997] | Phase 1/Phase 2 | 36 participants (Actual) | Interventional | 2019-06-06 | Active, not recruiting | ||
A Single Dose Open-Label Relative Bioavailability Study Comparing Two Capsule And A Solution Formulation Of PD-0332991 To The PD-0332991 Isethionate Capsule In Healthy Volunteers [NCT01602887] | Phase 1 | 24 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Molecular Profiling of Advanced Soft-tissue Sarcomas. A Phase III Study [NCT03784014] | Phase 3 | 960 participants (Anticipated) | Interventional | 2019-10-19 | Recruiting | ||
Neoadjuvant With Trastuzumab, Pyrotinib Plus Palbociclib and Fulvestrant in HER2-positive, ER-positive Breast Cancer [NCT05076695] | Phase 2 | 37 participants (Anticipated) | Interventional | 2021-10-15 | Recruiting | ||
A Phase 1 Dose Escalation and Expansion Open-label, Multicenter, Study of OP-1250 in Combination With the CDK4/6 Inhibitor Palbociclib in Adult Subjects With Advanced or Metastatic HR-positive, HER2-negative Breast Cancer [NCT05266105] | Phase 1 | 30 participants (Anticipated) | Interventional | 2021-12-10 | Recruiting | ||
Efficacy and Safety of Precision Therapy in Refractory Tumor (Long March Pathway) [NCT03239015] | Phase 2 | 300 participants (Anticipated) | Interventional | 2017-01-01 | Recruiting | ||
A Phase 1 Dose Escalation Study Evaluating the Safety and Tolerability of PF-06804103 in Patients With Human Epidermal Growth Factor Receptor 2 (HER2) Positive and Negative Solid Tumors [NCT03284723] | Phase 1 | 95 participants (Actual) | Interventional | 2017-11-01 | Completed | ||
A Single Arm Phase II Study of Palbociclib in Combination With Tamoxifen as First Line Therapy for Metastatic Hormone Receptor Positive Breast Cancer: Big Ten Cancer Research Consortium BTCRC-BRE15-016 [NCT02668666] | Phase 2 | 49 participants (Actual) | Interventional | 2016-06-30 | Active, not recruiting | ||
Efficacy and Safety of PD-0332991 in Patients With Advanced Gastrointestinal Stromal Tumors Refractory to Imatinib and Sunitinib: A Phase 2 Study [NCT01907607] | Phase 2 | 29 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
A Two-Part Study Evaluating the Combination of Tazemetostat and CPX-351 (Part 1) and Palbociclib With CPX-351 (Part 2) for the Treatment of Relapsed or Refractory Acute Myeloid Leukemia [NCT05627232] | Phase 1 | 24 participants (Anticipated) | Interventional | 2023-08-28 | Recruiting | ||
Palbociclib and Endocrine Therapy for LObular Breast Cancer Preoperative Study (PELOPS): A Randomized Phase II Study of Palbociclib With Letrozole Versus Letrozole Alone for Invasive Lobular Carcinoma and Invasive Ductal Carcinoma [NCT02764541] | Phase 2 | 195 participants (Actual) | Interventional | 2016-05-24 | Active, not recruiting | ||
Study to Investigate Outcome of Individualized Treatment Based on Pharmacogenomic Profiling & Ex Vivo Drug Sensitivity Testing of Patient-derived Organoids in Patients With Metastatic Colorectal Cancer [NCT05725200] | Phase 2 | 40 participants (Anticipated) | Interventional | 2022-09-27 | Recruiting | ||
Real-world Treatment Patterns and Effectiveness of Palbociclib in Combination With an Aromatase Inhibitor as Initial Endocrine Based Therapy in Metastatic/Advanced Breast Cancer [NCT04176354] | 1 participants (Actual) | Observational | 2019-01-25 | Active, not recruiting | |||
NCI-COG Pediatric MATCH (Molecular Analysis for Therapy Choice) - Phase 2 Subprotocol of Palbociclib in Patients With Tumors Harboring Activating Alterations in Cell Cycle Genes [NCT03526250] | Phase 2 | 23 participants (Actual) | Interventional | 2018-08-13 | Active, not recruiting | ||
A Phase 2 Trial to Evaluate the Safety and Efficacy of NKT2152 in Combination With Palbociclib (Doublet) and With Palbociclib and Sasanlimab (Triplet) in Subjects With Advanced or Metastatic Clear Cell Renal Cell Carcinoma [NCT05935748] | Phase 2 | 172 participants (Anticipated) | Interventional | 2023-07-28 | Recruiting | ||
A Phase 1b/2, Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Patients With Metastatic Breast Cancer [NCT05563220] | Phase 1/Phase 2 | 322 participants (Anticipated) | Interventional | 2023-01-24 | Recruiting | ||
A Randomized, Multicenter, Double-blind Phase 3 Study of Amcenestrant (SAR439859) Plus Palbociclib Versus Letrozole Plus Palbociclib for the Treatment of Patients With ER (+), HER2 (-) Breast Cancer Who Have Not Received Prior Systemic Anti-cancer Treatme [NCT04478266] | Phase 3 | 1,068 participants (Actual) | Interventional | 2020-10-14 | Terminated(stopped due to The study was terminated based on the review by an independent data monitoring committee of the prespecified interim analysis of the Phase 3 AMEERA-5 efficacy data. No new safety signals were observed.) | ||
A Phase 1/2, Open-label, Multicenter Study to Evaluate the Safety, Tolerability, Preliminary Antitumor Activity, Pharmacokinetics, and Pharmacodynamics of ZB716 as Monotherapy and in Combination With Palbociclib in Patients With Estrogen Receptor-Positive [NCT04669587] | Phase 1/Phase 2 | 106 participants (Anticipated) | Interventional | 2021-07-26 | Recruiting | ||
Phase II Neoadjuvant Study of Letrozole in Combination With PD0332991 (Oral CDK 4/6 Inhibitor) for ER Positive, HER2 Negative Breast Cancer in Postmenopausal Women [NCT01709370] | Phase 2 | 45 participants (Anticipated) | Interventional | 2012-02-29 | Recruiting | ||
Combination of MEK Inhibitor Binimetinib and CDK4/6 Inhibitor Palbociclib in KRAS and NRAS Mutant Metastatic Colorectal Cancers [NCT03981614] | Phase 2 | 102 participants (Actual) | Interventional | 2019-10-29 | Active, not recruiting | ||
A Phase Ia/Ib, Multicenter, Open-Label, Dose Escalation, Dose Expansion Study Evaluating the Safety, Pharmacokinetics, and Activity of GDC-9545 Alone or in Combination With Palbociclib and/or LHRH Agonist in Patients With Locally Advanced or Metastatic Es [NCT03332797] | Phase 1 | 181 participants (Actual) | Interventional | 2017-11-27 | Active, not recruiting | ||
A Phase One Open-Label Single-Radiolabeled Dose Study To Investigate The Absorption, Metabolism, And Excretion Of [14C] PD-0332991 In Healthy Male Volunteers [NCT01756768] | Phase 1 | 6 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
A Phase 1 Randomized, Open-Label, 2-Sequence, 2-Period Crossover Study Of The Effect Of Multiple Doses Of PD-0332991 On Midazolam Pharmacokinetics In Healthy Women of Non-Childbearing Potential [NCT01756781] | Phase 1 | 26 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
A Phase 1, Single Dose, Fixed Sequence, 2-Period Cross-Over Absolute Oral Bioavailability Study In Healthy Volunteers Comparing Oral To Intravenous Administration Of PD-0332991 [NCT01802476] | Phase 1 | 14 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
A Phase 1, Open-Label 4 Sequence 4 Period Crossover Study In Healthy Volunteers To Estimate The Effect Of Active Pharmaceutical Ingredient Particle Size And Lubrication On The Bioavailability Of A Single 125 Mg Dose Of Palbociclib (PD-0332991) Administere [NCT01844323] | Phase 1 | 24 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
A Phase II Study of PD 0332991 in Patients With Recurrent Rb Positive Glioblastoma [NCT01227434] | Phase 2 | 23 participants (Actual) | Interventional | 2010-09-30 | Terminated | ||
Phase II Safety Study of Palbociclib in Combination With Letrozole or Fulvestrant in African American Women With Hormone Receptor Positive HER2 Negative Advanced Breast Cancer [NCT02692755] | Phase 2/Phase 3 | 35 participants (Actual) | Interventional | 2016-09-30 | Completed | ||
A First-in-Human Study of PI3Kα Inhibitor, RLY-5836, in Combination With Targeted and Endocrine Therapies in Participants With Advanced Breast Cancer and as a Single Agent in Advanced Solid Tumors [NCT05759949] | Phase 1 | 265 participants (Anticipated) | Interventional | 2023-03-29 | Recruiting | ||
A Phase I, Open-Label Study of D-0502 Single Agent and D-0502 in Combination With Palbociclib in Women With Advanced or Metastatic ER-Positive and HER2-Negative Breast Cancer [NCT03471663] | Phase 1 | 200 participants (Actual) | Interventional | 2018-03-18 | Active, not recruiting | ||
A Multi-Center Open Label Single Arm Phase II Trial Evaluating the Efficacy of Palbociclib in Combination With Carboplatin for the Treatment of Unresectable Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma [NCT03194373] | Phase 2 | 21 participants (Actual) | Interventional | 2017-10-12 | Completed | ||
A Randomized, Multicenter, Open-Label, Two-Arm, Phase II, Neoadjuvant Study Evaluating the Efficacy, Safety, and Pharmacokinetics of GDC-9545 Plus Palbociclib Compared With Anastrozole Plus Palbociclib for Postmenopausal Women With Estrogen Receptor-Posit [NCT04436744] | Phase 2 | 221 participants (Actual) | Interventional | 2020-09-04 | Completed | ||
A Phase 1b/2, Protocol Evaluating the Safety, Tolerability, Pharmacokinetics, and Efficacy of Sotorasib Monotherapy and in Combination With Other Anti-cancer Therapies in Subjects With Advanced Solid Tumors With KRAS p.G12C Mutation (CodeBreak 101) [NCT04185883] | Phase 1/Phase 2 | 1,143 participants (Anticipated) | Interventional | 2019-12-17 | Recruiting | ||
Analysis of the Real-world Prescription Pattern of Palbociclib Combination Therapy With Aromatase Inhibitor as a 1st Line Therapy in Metastatic Breast Cancer Patients Using the National Health Insurance Claims Data in South Korea [NCT05132101] | 1 participants (Actual) | Observational | 2021-12-20 | Active, not recruiting | |||
Phase II Safety Single-arm Study of CDK4/6 Inhibition With Palbociclib in Hospitalized, Moderate COVID-19 Cases to Prevent Thromboinflammation [NCT05371275] | Phase 2 | 0 participants (Actual) | Interventional | 2022-04-21 | Withdrawn(stopped due to Study was withdrawn due to challenges in patient enrollment) | ||
Palbociclib Induced Neutropenia; Risk Factors and Treatment Outcome in Metastatic Breast Cancer Patients [NCT06076772] | 54 participants (Anticipated) | Observational [Patient Registry] | 2023-11-30 | Not yet recruiting | |||
Safety and Oversight of the Individually Tailored Treatment Approach: A Novel Pilot Study [NCT04801966] | 3 participants (Actual) | Interventional | 2021-09-23 | Terminated(stopped due to low recruitment) | |||
Patterns of Prescribing and Monitoring of Palbociclib [NCT03285568] | 67 participants (Actual) | Observational | 2015-02-03 | Completed | |||
A Phase 1b/2 Study of Agents Targeting the Mitogen-Activated Protein Kinase Pathway in Patients With Advanced Gastrointestinal Malignancies (HERKULES-3) [NCT05039177] | Phase 1/Phase 2 | 200 participants (Anticipated) | Interventional | 2021-09-20 | Recruiting | ||
A Phase I and Pharmacodynamic Trial of Timed Sequential Administration of the Cyclin Dependent Kinase 4/6 Inhibitor PD 0332991 Followed by Cytarabine Plus Mitoxantrone for Adults With Relapsed and Refractory Acute Leukemias and High-Risk Myelodysplasias [NCT01701375] | Phase 1 | 2 participants (Actual) | Interventional | 2012-09-30 | Terminated(stopped due to Material sponsor withdrew support) | ||
A Phase Ib/II Study of Palbociclib in Combination With Bazedoxifene in Hormone Receptor Positive Breast Cancer [NCT02448771] | Phase 1/Phase 2 | 36 participants (Actual) | Interventional | 2015-07-09 | Completed | ||
A Multicenter, Open-label, Phase Ib Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of CYH33 in Combination With Endocrine Therapy With or Without Palbociclib in Patients With PIK3CA Mutant, HR+, HER2- Advanced Breast [NCT04856371] | Phase 1 | 228 participants (Anticipated) | Interventional | 2021-04-30 | Not yet recruiting | ||
Analysis of Therapy Sequence in Women With Hormone Receptor-positive, HER2-negative Metastatic Breast Cancer in Russia: A Multicentre Retrospective Observational Real-life Study. [NCT04852081] | 1,000 participants (Anticipated) | Observational | 2021-01-01 | Recruiting | |||
A Phase 1/2 Study for the Safety, Efficacy, Pharmacokinetic and Pharmacodynamics Evaluation of Amcenestrant (SAR439859), Administered Orally as Monotherapy, Then in Combination With Other Anti-cancer Therapies in Postmenopausal Women With Estrogen Recepto [NCT03284957] | Phase 1/Phase 2 | 136 participants (Actual) | Interventional | 2017-09-20 | Active, not recruiting | ||
A Randomized, Multicenter, Open-label, Phase II Trial to Evaluate the Efficacy and Safety of Palbociclib in Combination With Fulvestrant or Letrozole in Patients With HER2 Negative, ER+ Metastatic Breast Cancer [NCT02491983] | Phase 2 | 486 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
A Phase Ib Trial Evaluating the Safety of Copanlisib, Letrozole, and Palbociclib in Metastatic Breast Cancer and Phase II Trial Comparing the Molecular Effects of Neoadjuvant Copanlisib in Combination With Palbociclib and Letrozole, vs. Copanlisib With Le [NCT03128619] | Phase 1 | 10 participants (Actual) | Interventional | 2017-08-02 | Terminated(stopped due to Insufficient accrual) | ||
Phase II Multicenter Trial of Palbociclib in Second Line of Advanced Sarcomas With CDK4 Overexpression. [NCT03242382] | Phase 2 | 40 participants (Anticipated) | Interventional | 2017-03-31 | Recruiting | ||
A Phase I, Open-Label, Dose-Escalation Study Evaluating the Safety, Tolerability, and Pharmacokinetics of GDC-0077 as a Single Agent in Patients With Locally Advanced or Metastatic PIK3CA-Mutant Solid Tumors and in Combination With Endocrine and Targeted [NCT03006172] | Phase 1 | 256 participants (Anticipated) | Interventional | 2016-12-13 | Recruiting | ||
A Phase I Study of Avelumab, Palbociclib, and Cetuximab in Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma [NCT03498378] | Phase 1 | 24 participants (Anticipated) | Interventional | 2018-06-06 | Active, not recruiting | ||
PHASE 1/2 OPEN-LABEL STUDY OF PF-06747775 (EPIDERMAL GROWTH FACTOR RECEPTOR T790M INHIBITOR) IN PATIENTS WITH ADVANCED EPIDERMAL GROWTH FACTOR RECEPTOR MUTANT (DEL 19 OR L858R ± T790M) NON-SMALL CELL LUNG CANCER [NCT02349633] | Phase 1/Phase 2 | 65 participants (Actual) | Interventional | 2015-05-14 | Terminated(stopped due to "The study was ended for strategic reasons and changes in the external environment.~The safety profile and risk benefit ratio for PF-0674775 remained unchanged.") | ||
Observational Analysis of Treatment With Palbociclib in Patients With Locally Advanced and / or Metastatic RH + / HER 2- Breast Cancer in the First Line of Treatment Within Routine Clinical Practice. [NCT04874025] | 815 participants (Actual) | Observational | 2021-07-31 | Completed | |||
A Randomized Phase II Study of Androgen Deprivation Therapy With or Without Palbociclib in RB-Positive Metastatic Hormone-Sensitive Prostate Cancer [NCT02059213] | Phase 2 | 72 participants (Actual) | Interventional | 2014-06-30 | Completed | ||
A Phase Ib Trial of Fulvestrant, Palbociclib (CDK4/6 Inhibitor) and Erdafitinib (JNJ- 42756493,Pan-FGFR Tyrosine Kinase Inhibitor) in ER+/HER2-/FGFR-Amplified Metastatic Breast Cancer (MBC) [NCT03238196] | Phase 1 | 35 participants (Actual) | Interventional | 2017-08-18 | Active, not recruiting | ||
An Open-label, Prospective Study of Tumor Response Time of Palbociclib in Combination With AI in Real-world First-line Treatment of Postmenopausal Chinese Patients With ER (+) HER2 (-) Metastatic Breast Cancer [NCT04858997] | Phase 2 | 150 participants (Anticipated) | Interventional | 2021-04-22 | Recruiting | ||
PIPA: A Phase Ib Study to Assess the Safety, Tolerability and Efficacy of the PI3K Inhibitors, Taselisib (GDC-0032) or Pictilisib (GDC-0941), in Combination With PAlbociclib, With the Subsequent Addition of Fulvestrant in PIK3CA-mutant Breast Cancers [NCT02389842] | Phase 1 | 93 participants (Anticipated) | Interventional | 2015-03-25 | Active, not recruiting | ||
Phase II Study of the Combination of Pembrolizumab, Letrozole, and Palbociclib in Postmenopausal Patients With Newly Diagnosed Metastatic Estrogen Receptor Positive Breast Cancer [NCT02778685] | Phase 2 | 40 participants (Actual) | Interventional | 2016-09-30 | Active, not recruiting | ||
Phase II Trial of Palbociclib (PD-0332991) in Patients With Metastatic Urothelial Cancer (UC) After Failure of First-Line Chemotherapy [NCT02334527] | Phase 2 | 12 participants (Actual) | Interventional | 2015-03-17 | Terminated(stopped due to Data from first 12 subjects-primary endpoint not met. Data analysis underway.) | ||
Phase 2 Trial of Palbociclib and Ganitumab in Patients With Relapsed or Refractory Ewing Sarcoma [NCT04129151] | Phase 2 | 10 participants (Actual) | Interventional | 2019-12-05 | Completed | ||
ENGOT-EN3-NSGO/PALEO: A Randomized, Double-blind, Placebo-controlled, Phase II Trial of Palbociclib in Combination With Letrozole Versus Placebo in Combination With Letrozole for Patients With Estrogen Receptor Positive Advanced or Recurrent Endometrial C [NCT02730429] | Phase 2 | 78 participants (Actual) | Interventional | 2017-02-15 | Completed | ||
A STUDY OF PALBOCICLIB IN COMBINATION WITH LETROZOLE AS TREATMENT OF POST-MENOPAUSAL WOMEN WITH HORMONE RECEPTOR-POSITIVE, HER2-NEGATIVE ADVANCED BREAST CANCER FOR WHOM LETROZOLE THERAPY IS DEEMED APPROPRIATE [NCT02679755] | Phase 4 | 252 participants (Actual) | Interventional | 2016-03-09 | Completed | ||
Clinical Trial to Evaluate Safety and Anti-tumor Activity of AKT Inhibitor, Ipatasertib,With Endocrine Therapy With/Without CDK 4/6 Inhibitor for Patients With Metastatic Hormone Receptor Positive Breast Cancer (TAKTIC) [NCT03959891] | Phase 1 | 77 participants (Actual) | Interventional | 2019-05-30 | Active, not recruiting | ||
A Phase III, Multicenter, Open-label Study of Ribociclib vs. Palbociclib in Patients With Advanced Hormone Receptor-positive/HER2-negative/HER2-Enriched Breast Cancer - HARMONIA Trial [NCT05207709] | Phase 3 | 456 participants (Anticipated) | Interventional | 2022-03-28 | Recruiting | ||
Samsung Medical Center [NCT03219554] | Phase 2 | 33 participants (Anticipated) | Interventional | 2017-08-31 | Not yet recruiting | ||
A Phase II Clinical Trial Assessing the Safety of Neoadjuvant Palbociclib in Combination With Endocrine Therapy for Post and Pre-menopausal Patients With Early Stage Hormone Receptor Positive and Her-2/Neu Negative Breast Cancer [NCT05069038] | Phase 2 | 46 participants (Anticipated) | Interventional | 2022-03-02 | Recruiting | ||
CIMER: Combined Immunotherapies in Metastatic ER+ Breast Cancer [NCT04563507] | Phase 2 | 102 participants (Anticipated) | Interventional | 2020-11-12 | Recruiting | ||
A PHASE 1/2 STUDY OF THE EFFICACY, SAFETY, AND PHARMACOKINETICS OF ORAL PD-0332991, A CYCLIN-DEPENDENT KINASE 4 AND 6 (CDK4/6) INHIBITOR, AS SINGLE AGENT IN JAPANESE PATIENTS WITH ADVANCED SOLID TUMORS OR IN COMBINATION WITH LETROZOLE FOR THE FIRST-LINE T [NCT01684215] | Phase 2 | 61 participants (Actual) | Interventional | 2012-10-19 | Completed | ||
PHASE 1B STUDY TO ASSESS THE SAFETY, TOLERABILITY, AND CLINICAL ACTIVITY OF GEDATOLISIB IN COMBINATION WITH PALBOCICLIB AND EITHER LETROZOLE OR FULVESTRANT IN WOMEN WITH METASTATIC OR LOCALLY ADVANCED/RECURRENT BREAST CANCER (MBC) [NCT02684032] | Phase 1 | 141 participants (Actual) | Interventional | 2016-06-14 | Completed | ||
Neoadjuvant Biomarker ResearcH Study of Palbociclib Combined With Endocrine Therapy in Estrogen Receptor Positive/HER2 Negative Breast CAncer [NCT03065621] | Phase 2 | 100 participants (Actual) | Interventional | 2017-07-05 | Completed | ||
A Phase II Multi-Institutional Study of Concurrent Radiotherapy, Palbociclib, and Hormone Therapy for Treatment of Bone Metastasis in Breast Cancer Patients [NCT03691493] | Phase 2 | 38 participants (Actual) | Interventional | 2019-02-08 | Completed | ||
INTERACT- Integrated Evaluation of Resistance and Actionability Using Circulating Tumor DNA in HR Positive Metastatic Breast Cancers [NCT04256941] | Phase 2 | 4 participants (Actual) | Interventional | 2019-05-31 | Completed | ||
Comparative Effectiveness of Palbociclib Based-therapy as Initial Endocrine Therapy Versus Palbociclib Based-therapy After Chemotherapy for HR+/HER2- Advanced Breast Cancer in Chinese Clinical Practice: a Real-world Study [NCT05343117] | 400 participants (Anticipated) | Observational | 2021-12-01 | Recruiting | |||
Palbociclib in Combination With Letrozole in Patients With Hormone Receptor (HR) Positive/Human Epidermal Growth Factor Receptor 2 (HER2) Negative Residual Disease After Standard Neoadjuvant Chemotherapy (PROMETEO II) [NCT04130152] | Early Phase 1 | 22 participants (Actual) | Interventional | 2019-11-21 | Completed | ||
Comparative Assessment of Overall Survival in Medicare Patients With HR+/HER2- Metastatic Breast Cancer Treated With Palbociclib in Combination With Aromatase Inhibitor (AI vs. AI Alone) [NCT06086340] | 782 participants (Anticipated) | Observational | 2023-09-29 | Active, not recruiting | |||
A First-in-Human Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, as a Single Agent in Advanced Solid Tumor Patients and in Combination With Fulvestrant in Patients With Advanced Breast Cancer [NCT05216432] | Phase 1 | 400 participants (Anticipated) | Interventional | 2021-12-08 | Recruiting | ||
A Phase I Trial of Palbociclib in Combination With Dexamethasone in Relapsed or Refractory Adult B-Cell Acute Lymphoblastic Leukemia (ALL) [NCT03472573] | Phase 1 | 7 participants (Actual) | Interventional | 2018-05-09 | Completed | ||
Platform Study of Genotyping Guided Precision Medicine for Rare Tumors in China [NCT04423185] | Phase 2 | 770 participants (Anticipated) | Interventional | 2020-08-15 | Not yet recruiting | ||
Evaluate Efficacy and Safety of CDK4/6 Inhibitor Palbociclib in Combination With Fulvestrant Versus Fulvestrant in Female Patients With HR+/HER2- Advanced Breast Cancer: A Real-world Multicenter Observational Study in China [NCT04526028] | 612 participants (Anticipated) | Observational | 2019-09-13 | Recruiting | |||
A Histology-Independent Study of the Cyclin Inhibitor Palbociclib in Patients With Advanced Cancer Harboring Aberrations in the Cyclin Pathway [NCT03123744] | Phase 2 | 0 participants (Actual) | Interventional | 2018-07-01 | Withdrawn(stopped due to No study funding available.) | ||
Phase Ib IIT of Heat Shock Protein 90 Inhibitor TAS-116 Combined With Cyclin-dependent Kinase 4/6 Inhibitor Palbociclib in Advanced Breast Cancer Progressing on Palbociclib & Treatment-refractory Solid Tumors With Retinoblastoma Deficiency [NCT05655598] | Phase 1 | 27 participants (Anticipated) | Interventional | 2023-09-12 | Recruiting | ||
A Phase I/II Dose Escalation Study of the CDK4/6 Inhibitor, Palbociclib in Combination With Cetuximab and Intensity Modulated Radiation Therapy (IMRT) for Locally Advanced Squamous Cell Carcinoma of the Head and Neck [NCT03024489] | Phase 1/Phase 2 | 27 participants (Actual) | Interventional | 2017-07-19 | Active, not recruiting | ||
Official Title A Randomized Phase 2 Trial With a Safety Lead-In to Evaluate Palbociclib Versus Palbociclib and Cemiplimab for the Treatment of Advanced Dedifferentiated Liposarcoma [NCT05694871] | Phase 2 | 72 participants (Anticipated) | Interventional | 2023-05-30 | Suspended(stopped due to Scheduled analysis of safety lead in.) | ||
Preoperative Palbociclib in Patients With DCIS of the Breast That Are Candidates for Surgery [NCT03535506] | Phase 2 | 17 participants (Actual) | Interventional | 2018-10-08 | Active, not recruiting | ||
A Proof of Concept Study to Explore Safety and Efficacy of Tri-therapy Approach in Advanced/Metastatic NSCLC and Retrospectively Assess the Ability of Integrated Genomics and Transcriptomics to Match Patients to the Combination [NCT03386929] | Phase 1/Phase 2 | 15 participants (Actual) | Interventional | 2017-11-29 | Terminated(stopped due to The SPRING trial had to be early terminated at the end of the Phase 1 portion of the study due to the absence of funding necessary for the performance of the Phase 2.) | ||
NCI-COG Pediatric MATCH (Molecular Analysis for Therapy Choice) Screening Protocol [NCT03155620] | Phase 2 | 2,316 participants (Anticipated) | Interventional | 2017-07-31 | Recruiting | ||
Retrospective, Multicenter, Observational Study to Evaluate Real-World Effectiveness of Palbociclib Plus Endocrine Therapy in Japanese Patients With HR+/HER2- Advanced Breast Cancer in First Line or Second Line Settings [NCT05399329] | 688 participants (Actual) | Observational | 2022-04-20 | Active, not recruiting | |||
A PHASE 1 OPEN-LABEL PHARMACOKINETICS STUDY OF PALBOCICLIB, A CYCLIN-DEPENDENT KINASE 4 AND 6 (CDK4/6) INHIBITOR, IN POSTMENOPAUSAL CHINESE WOMEN WITH ER (+), HER2 (-) ADVANCED BREAST CANCER [NCT02499146] | Phase 1 | 26 participants (Actual) | Interventional | 2015-09-11 | Active, not recruiting | ||
Description of Treatment Patterns and Description and Comparison of Healthcare Resource Utilization and Costs of Women With Metastatic HR+/HER2- Breast Cancer Treated With CDK4/6 Inhibitors [NCT05153135] | 4,320 participants (Actual) | Observational | 2020-05-08 | Completed | |||
Phase 1B Study of PD-0332991 in Combination With T-DM1 in the Treatment of Patients With Advanced HER2 (Human Epidermal Growth Factor Receptor 2)-Positive Breast Cancer [NCT01976169] | Phase 1 | 29 participants (Actual) | Interventional | 2014-01-24 | Completed | ||
A Randomized Phase II Trial of Fulvestrant and Palbociclib in Combination With Copanlisib (FPC) Versus Fulvestrant and Palbociclib Alone (FP) for Endocrine Resistant, Hormone Receptor Positive, HER2 Negative Metastatic Breast Cancer (FPC vs FP) [NCT03377101] | Phase 2 | 0 participants (Actual) | Interventional | 2018-08-07 | Withdrawn(stopped due to change in study design.) | ||
A Phase II Study of CDK4/6 Inhibition (Palbociclib) Combined With PD-1 Blockade (INCMGA00012) in Patients With Advanced Well-differentiated Dedifferentiated Liposarcoma [NCT04438824] | Phase 2 | 42 participants (Anticipated) | Interventional | 2020-06-17 | Recruiting | ||
A Phase I Trial of Ibrutinib Plus PD 0332991 (Palbociclib) in Patients With Previously Treated Mantle Cell Lymphoma [NCT02159755] | Phase 1 | 28 participants (Actual) | Interventional | 2014-05-20 | Active, not recruiting | ||
A Randomised Trial of Early Detection of Molecular Relapse With Circulating Tumour DNA Tracking and Treatment With Palbociclib Plus Fulvestrant Versus Standard Endocrine Therapy in Patients With ER Positive HER2 Negative Breast Cancer [NCT04985266] | Phase 2 | 1,100 participants (Anticipated) | Interventional | 2022-03-30 | Recruiting | ||
A Phase 1b/2, Open Label, Dose Escalation and Expansion Study of the Glutaminase Inhibitor Telaglenastat (CB-839) in Combination With CDK4/6 Inhibitor Palbociclib in Patients With Advanced or Metastatic Solid Tumors [NCT03965845] | Phase 1/Phase 2 | 53 participants (Actual) | Interventional | 2019-06-25 | Completed | ||
Phase I Dose-Escalation Study of Combination of Gedatolisib (a Dual Inhibitor of PI3-K and mTOR) With Palbociclib and Faslodex in the Neoadjuvant Setting in Previously Untreated Patients With ER+/HER2- Breast Cancer [NCT02626507] | Phase 1 | 18 participants (Anticipated) | Interventional | 2016-01-31 | Active, not recruiting | ||
A RANDOMIZED, MULTICENTER, DOUBLE-BLIND PHASE 3 STUDY OF PD-0332991 (ORAL CDK 4/6 INHIBITOR) PLUS LETROZOLE VERSUS PLACEBO PLUS LETROZOLE FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN WITH ER (+), HER2 (-) BREAST CANCER WHO HAVE NOT RECEIVED ANY PRIOR SYSTEMI [NCT01740427] | Phase 3 | 666 participants (Actual) | Interventional | 2013-02-22 | Completed | ||
A Phase 1, Open-Label, Multicenter Study to Assess the Safety, Tolerability, Pharmacokinetics, and Preliminary Antitumor Activity of Ascending Doses of G1T48 Alone and in Combination With Palbociclib in Women With Estrogen Receptor-Positive, HER2-Negative [NCT03455270] | Phase 1 | 107 participants (Actual) | Interventional | 2018-05-09 | Completed | ||
A Phase 1 Study of Palbociclib in Combination With Cisplatin or Carboplatin in Advanced Solid Malignancies [NCT02897375] | Phase 1 | 71 participants (Actual) | Interventional | 2016-10-24 | Completed | ||
Phase I Study of CDK 4-6 Inhibitor PD-0332991 (Palbociclib; IBRANCE) in Children With Recurrent, Progressive or Refractory Central Nervous System Tumors [NCT02255461] | Phase 1 | 35 participants (Actual) | Interventional | 2014-12-08 | Terminated(stopped due to Data for the primary objectives is complete and the MTD identified in Stratum II.) | ||
Palbociclib Treatment Patterns in Swedish Patients With Metastatic Breast Cancer - Swedish Ibrance Registries Insights (SIRI) [NCT04654208] | 1,500 participants (Anticipated) | Observational | 2020-12-15 | Recruiting | |||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |