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Assay Detail

CHEMBL4841253

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of CDK9/cyclin T1 (unknown origin) incubated for 2 hrs in presence of ATP by FRET based LANCE assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

CDK9/cyclin T1 (CHEMBL2111389)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.
Han X, Song N, Saidahmatov A, Wang P, Wang Y, Hu X, Kan W, Zhu W, Gao L, Zeng M, Wang Y, Li C, Li J, Liu H, Zhou Y, Wang J.
J Med Chem (2021) 64 : 14647 -14663
PubMed 34477384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.02 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4786559 1 8.30
CHEMBL4876497 1 8.27
CHEMBL4856767 1 8.22
CHEMBL4875272 1 8.18
CHEMBL4872952 1 8.04
CHEMBL4855785 1 7.85
CHEMBL4860265 1 7.69
CHEMBL4857229 1 7.68
CHEMBL4848043 1 7.62
CHEMBL4871323 1 7.61
CHEMBL4864763 1 7.58
CHEMBL4856958 1 7.56
CHEMBL4862568 1 7.37
CHEMBL4874951 1 7.30
CHEMBL4858120 1 7.12
CHEMBL4866369 1 6.82
CHEMBL4865258 1 6.47
CHEMBL4867494 1 6.20
CHEMBL4863726 1 6.19
CHEMBL4861326 1 6.11
CHEMBL4852806 1 6.05
CHEMBL4863744 1 6.00
CHEMBL4870617 1 5.17
CHEMBL4870732 1 5.06
CHEMBL4859084 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4786559 IC50 = 4.96 nM 8.30
CHEMBL4876497 IC50 = 5.41 nM 8.27
CHEMBL4856767 IC50 = 6.04 nM 8.22
CHEMBL4875272 IC50 = 6.57 nM 8.18
CHEMBL4872952 IC50 = 9.15 nM 8.04
CHEMBL4855785 IC50 = 14.21 nM 7.85
CHEMBL4860265 IC50 = 20.42 nM 7.69
CHEMBL4857229 IC50 = 20.75 nM 7.68
CHEMBL4848043 IC50 = 24.25 nM 7.62
CHEMBL4871323 IC50 = 24.69 nM 7.61
CHEMBL4864763 IC50 = 26.52 nM 7.58
CHEMBL4856958 IC50 = 27.29 nM 7.56
CHEMBL4862568 IC50 = 42.3 nM 7.37
CHEMBL4874951 IC50 = 50.28 nM 7.30
CHEMBL4858120 IC50 = 75.61 nM 7.12
CHEMBL4866369 IC50 = 152.77 nM 6.82
CHEMBL4865258 IC50 = 341.35 nM 6.47
CHEMBL4867494 IC50 = 633.35 nM 6.20
CHEMBL4863726 IC50 = 642.95 nM 6.19
CHEMBL4861326 IC50 = 773.85 nM 6.11
CHEMBL4852806 IC50 = 882.8 nM 6.05
CHEMBL4863744 IC50 = 994.85 nM 6.00
CHEMBL4870617 IC50 = 6799.0 nM 5.17
CHEMBL4870732 IC50 = 8769.0 nM 5.06
CHEMBL4859084 IC50 = 8925.0 nM 5.05