4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide: a protein kinase inhibitor; structure in first source [MeSH]
ID Source | ID |
---|---|
PubMed CID | 44595079 |
CHEMBL ID | 4116008 |
SCHEMBL ID | 736734 |
MeSH ID | M000602453 |
Synonym |
---|
S3566 |
cerdulatinib |
cerdulatinib [inn] |
D1LXQ45S1O , |
5-pyrimidinecarboxamide, 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)-1-piperazinyl)phenyl)amino)- |
4-(cyclopropylamino)-2-((4-(4-(ethanesulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide |
prt-062070 |
1198300-79-6 |
cerdulatinib [who-dd] |
rvt-502 |
HY-15999 |
CS-3329 |
SCHEMBL736734 |
unii-d1lxq45s1o |
cerdulatinib (prt062070) |
AC-30243 |
prt062070 |
prt 062070 |
4-(cyclopropylamino)-2-[4-(4-ethylsulfonylpiperazin-1-yl)anilino]pyrimidine-5-carboxamide |
gtpl8957 |
prt-2070 |
AKOS026750510 |
prt2070 |
4-(cyclopropylamino)-2-({4-[4-(ethanesulfonyl)piperazin-1-yl]phenyl}amino)pyrimidine-5-carboxamide |
NCGC00386415-04 |
FT-0741914 |
4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide |
cerdulatinib; prt062070; prt2070 |
EX-A2143 |
DB15499 |
Q27075860 |
prt2070; prt-2070; prt 2070; prt-062070; prt 062070; prt062070 |
BCP10681 |
SB16931 |
CHEMBL4116008 , |
4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide |
cerdulatinib (prt2070) |
YXB30079 |
C71670 |
DTXSID001115521 |
AS-56368 |
bdbm50468574 |
nsc825827 |
nsc800071 |
nsc-825827 |
nsc-800071 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
PPM1D protein | Homo sapiens (human) | Potency | 2.6212 | AID1347411 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 26.8370 | AID1645841 |
G | Vesicular stomatitis virus | Potency | 18.9991 | AID1645842 |
Interferon beta | Homo sapiens (human) | Potency | 6.7157 | AID1347411; AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 18.9991 | AID1645842 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 18.9991 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 18.9991 | AID1645842 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
NUAK family SNF1-like kinase 1 | Homo sapiens (human) | IC50 | 0.0040 | AID1845556 |
Tyrosine-protein kinase JAK2 | Homo sapiens (human) | IC50 | 0.0060 | AID1405293; AID1875944 |
Tyrosine-protein kinase JAK1 | Homo sapiens (human) | IC50 | 0.0120 | AID1405292; AID1875947 |
Tyrosine-protein kinase JAK3 | Homo sapiens (human) | IC50 | 0.0080 | AID1405291; AID1875945 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
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 ISSN: 1091-6490 | 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
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 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347415 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
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 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1875945 | Inhibition of JAK 3 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 ISSN: 1520-4804 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1405292 | Inhibition of JAK1 (unknown origin) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 ISSN: 1520-4804 | Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. |
AID1405293 | Inhibition of JAK2 (unknown origin) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 ISSN: 1520-4804 | Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. |
AID1405291 | Inhibition of JAK3 (unknown origin) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 ISSN: 1520-4804 | Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. |
AID1845556 | Inhibition of NUAK1 (unknown origin) | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 ISSN: 1520-4804 | Development and Therapeutic Potential of NUAKs Inhibitors. |
AID1875944 | Inhibition of JAK 2 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 ISSN: 1520-4804 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1875947 | Inhibition of JAK 1 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 ISSN: 1520-4804 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1345508 | Human colony stimulating factor 1 receptor (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345714 | Human Janus kinase 2 (Janus kinase (JakA) family) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345760 | Human mitogen-activated protein kinase kinase kinase 9 (MLK subfamily) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345744 | Human Janus kinase 3 (Janus kinase (JakA) family) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345876 | Human spleen associated tyrosine kinase (Syk family) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345757 | Human Janus kinase 1 (Janus kinase (JakA) family) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345885 | Human serine/threonine kinase 4 (MST subfamily) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345872 | Human tyrosine kinase 2 (Janus kinase (JakA) family) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
AID1345741 | Human NUAK family kinase 1 (NuaK subfamily) | 2014 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 351, Issue:3 ISSN: 1521-0103 | The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 9 (56.25) | 24.3611 |
2020's | 7 (43.75) | 2.80 |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 3 (18.75%) | 5.53% |
Reviews | 2 (12.50%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 11 (68.75%) | 84.16% |
Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
adenine | 6-aminopurines; purine nucleobase | Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one | organic heterotetracyclic compound; organofluorine compound | EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
pci 32765 | acrylamides; aromatic amine; aromatic ether; N-acylpiperidine; pyrazolopyrimidine; tertiary carboxamide | antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
incb-018424 | nitrile; pyrazoles; pyrrolopyrimidine | antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
piperidines | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
---|---|---|---|---|---|---|---|---|---|---|---|---|
2019 Novel Coronavirus Disease | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Acute Lymphoid Leukemia | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Adjuvant Arthritis | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
ATLL | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Autoimmune Diabetes | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
B-Cell Chronic Lymphocytic Leukemia | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
B-Cell Lymphoma | 0 | 2014 | 2019 | 6.7 | low | 2 | 0 | 0 | 0 | 3 | 0 | |
B-Cell Prolymphocytic Leukemia | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Cirrhosis | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Dermatitis, Atopic | 0 | 2021 | 2021 | 3.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
Diabetes Mellitus, Type 1 | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Diffuse Large B-Cell Lymphoma | 0 | 2015 | 2019 | 7.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
Diffuse Mixed Small and Large Cell Lymphoma | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Disease Exacerbation | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Disease Models, Animal | 0 | 2014 | 2020 | 7.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
Eczema, Atopic | 0 | 2021 | 2021 | 3.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
Fibrosis | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Hematologic Malignancies | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Hematologic Neoplasms | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Leukemia-Lymphoma, Adult T-Cell | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Leukemia, Lymphocytic, Chronic, B-Cell | 1 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Leukemia, Prolymphocytic, B-Cell | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Lymphoma, B-Cell | 0 | 2014 | 2019 | 6.7 | low | 2 | 0 | 0 | 0 | 3 | 0 | |
Lymphoma, Large B-Cell, Diffuse | 0 | 2015 | 2019 | 7.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
Lymphoma, Non-Hodgkin | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Precursor Cell Lymphoblastic Leukemia-Lymphoma | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Viral Diseases | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Virus Diseases | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
Article | Year |
---|---|
Cerdulatinib Pharmacodynamics and Relationships to Tumor Response Following Oral Dosing in Patients with Relapsed/Refractory B-cell Malignancies. Clinical cancer research : an official journal of the American Association for Cancer Research, , 02-15, Volume: 25, Issue:4 | 2019 |
Article | Year |
---|---|
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |
Article | Year |
---|---|
Cerdulatinib Pharmacodynamics and Relationships to Tumor Response Following Oral Dosing in Patients with Relapsed/Refractory B-cell Malignancies. Clinical cancer research : an official journal of the American Association for Cancer Research, , 02-15, Volume: 25, Issue:4 | 2019 |
Anti-adult T‑cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor. International journal of oncology, , Volume: 53, Issue:4 | 2018 |
The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. The Journal of pharmacology and experimental therapeutics, , Volume: 351, Issue:3 | 2014 |