CINK4: cyclin-dependent kinase 4 inhibitor; may have tumor suppression activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
ID Source | ID |
---|---|
PubMed CID | 24825971 |
CHEMBL ID | 1242367 |
CHEMBL ID | 2028998 |
CHEBI ID | 91456 |
SCHEMBL ID | 14334442 |
SCHEMBL ID | 14334441 |
SCHEMBL ID | 14040726 |
MeSH ID | M0384493 |
Synonym |
---|
CHEMBL1242367 , |
cgp-082996 |
bdbm50378824 |
HMS2043N19 |
NCGC00346952-01 |
cgp82996 |
CHEMBL2028998 , |
AKOS016358850 |
SCHEMBL14334442 |
SCHEMBL14334441 |
SCHEMBL14040726 |
CHEBI:91456 |
bdbm50503352 |
cink4, >=95% (hplc) |
359886-84-3 |
cdk4/6 inhibitor iv |
4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-5-indolyl]amino]-4-pyrimidinyl]amino]-1-cyclohexanol |
Q27163298 |
trans-4-((2-((1-benzyl-1h-indol-5-yl)amino)-6-(ethylamino)pyrimidin-4-yl)amino)cyclohexanol |
cdk4/6inhibitoriv |
cink4 |
4-[[2-[(1-benzylindol-5-yl)amino]-6-(ethylamino)pyrimidin-4-yl]amino]cyclohexan-1-ol |
CS-0133475 |
HY-136726 |
cgp-82996 |
rel-(1s,4s)-4-((2-((1-benzyl-1h-indol-5-yl)amino)-6-(ethylamino)pyrimidin-4-yl)amino)cyclohexan-1-ol |
Excerpt | Reference | Relevance |
---|---|---|
"CINK4 treatment resulted in statistically significantly (P: =.031) smaller mean tumor volumes in a mouse xenograft model." | ( Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. Chaudhuri, B; Fabbro, D; Fretz, H; Furet, P; Muller, L; O'Reilly, T; Soni, R; Stephan, C; Zumstein-Mecker, S, 2001) | 1.03 |
Excerpt | Reference | Relevance |
---|---|---|
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Class | Description |
---|---|
indoles | Any compound containing an indole skeleton. |
[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 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 27.6354 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
polyprotein | Zika virus | Potency | 33.1734 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
[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) |
---|---|---|---|---|---|---|---|
Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0010 | 0.5585 | 8.0000 | AID1513684 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 53.0667 | 0.0004 | 1.3452 | 10.0000 | AID1069268; AID1513678; AID512723 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | IC50 (µMol) | 4.3333 | 0.0006 | 0.5706 | 10.0000 | AID1069266; AID1513680; AID512719 |
G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 54.6000 | 0.0013 | 1.4518 | 10.0000 | AID1069268; AID1513678 |
Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 1.0339 | 10.0000 | AID1513681 |
G1/S-specific cyclin-D1 | Homo sapiens (human) | IC50 (µMol) | 5.7500 | 0.0006 | 0.5479 | 9.5000 | AID1069266; AID1513680 |
G1/S-specific cyclin-E1 | Homo sapiens (human) | IC50 (µMol) | 27.6000 | 0.0010 | 1.0404 | 10.0000 | AID1069267; AID1513679 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 28.8000 | 0.0004 | 1.0444 | 10.0000 | AID1069267; AID1513679; AID1513681; AID512724 |
Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.9106 | 9.2000 | AID1513683 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0010 | 0.6236 | 8.0000 | AID1513684 |
Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0005 | 1.0823 | 9.2000 | AID1513683 |
CDK-activating kinase assembly factor MAT1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0030 | 1.6892 | 9.2000 | AID1513683 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | IC50 (µMol) | 5.6000 | 0.0019 | 0.8654 | 7.2000 | AID512720 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 17.5000 | 0.0002 | 1.1832 | 10.0000 | AID1513682; AID512721 |
Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0010 | 1.2898 | 10.0000 | AID1513682 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1513744 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 1.7 to 19.8 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? |
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? |
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? |
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? |
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? |
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? |
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? |
AID1513694 | Induction of cell cycle arrest in human HCT116 cells assessed as reduction in accumulation at G1 phase at 1.7 to 19.8 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? |
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? |
AID1069268 | Inhibition of GST-tagged human CDK1/cyclinB expressed in sf9 cells using GST-pRb as substrate by [gamma-33P]ATP 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). |
AID512723 | Inhibition of CDK1 | 2006 | The AAPS journal, Mar-24, Volume: 8, Issue:1 | Selectivity and potency of cyclin-dependent kinase inhibitors. |
AID1069267 | Inhibition of GST-tagged human CDK2/cyclinE expressed in sf9 cells using GST-pRb as substrate by [gamma-33P]ATP 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). |
AID1069266 | Inhibition of GST-tagged human CDK4/cyclinD1 expressed in sf9 cells using GST-pRb as substrate by [gamma-33P]ATP 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). |
AID512724 | Inhibition of CDK2 | 2006 | The AAPS journal, Mar-24, Volume: 8, Issue:1 | Selectivity and potency of cyclin-dependent kinase inhibitors. |
AID512720 | Inhibition of CDK6 | 2006 | The AAPS journal, Mar-24, Volume: 8, Issue:1 | Selectivity and potency of cyclin-dependent kinase inhibitors. |
AID512721 | Inhibition of CDK5 | 2006 | The AAPS journal, Mar-24, Volume: 8, Issue:1 | Selectivity and potency of cyclin-dependent kinase inhibitors. |
AID512719 | Inhibition of CDK4 | 2006 | The AAPS journal, Mar-24, Volume: 8, Issue:1 | Selectivity and potency of cyclin-dependent kinase inhibitors. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
[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 | 3 (23.08) | 29.6817 |
2010's | 4 (30.77) | 24.3611 |
2020's | 6 (46.15) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 1 (7.69%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 12 (92.31%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |