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Assay Detail

CHEMBL5376175

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

Binding
Inhibition of human CDK9/Cyclin T1 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs
39
Total Activities
39
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

Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
Freeman DB, Hopkins TD, Mikochik PJ, Vacca JP, Gao H, Naylor-Olsen A, Rudra S, Li H, Pop MS, Villagomez RA, Lee C, Li H, Zhou M, Saffran DC, Rioux N, Hood TR, Day MAL, McKeown MR, Lin CY, Bischofberger N, Trotter BW.
J Med Chem (2023) 66 : 15629 -15647
PubMed 37967851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.17 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5440829 1 8.40
CHEMBL5199065 ISTISOCICLIB 2.0 1 8.22
CHEMBL5420915 1 8.22
CHEMBL5428866 1 8.05
CHEMBL5440226 1 8.00
CHEMBL5419715 1 8.00
CHEMBL5438063 1 7.92
CHEMBL5421527 1 7.85
CHEMBL5409780 1 7.70
CHEMBL5396123 1 7.68
CHEMBL5419691 1 7.60
CHEMBL5423100 1 7.60
CHEMBL5411270 1 7.40
CHEMBL5413258 1 7.37
CHEMBL5409162 1 7.34
CHEMBL5421587 1 7.33
CHEMBL5440331 1 7.30
CHEMBL5430225 1 7.26
CHEMBL5419772 1 7.13
CHEMBL5404877 1 7.10
CHEMBL5439995 1 7.09
CHEMBL5406720 1 7.04
CHEMBL5405502 1 7.04
CHEMBL5436706 1 7.02
CHEMBL5425977 1 6.98
CHEMBL5403832 1 6.97
CHEMBL5424203 1 6.93
CHEMBL5424511 1 6.81
CHEMBL5438393 1 6.75
CHEMBL5438750 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5440829 IC50 = 4.0 nM 8.40
CHEMBL5199065 ISTISOCICLIB IC50 = 6.0 nM 8.22
CHEMBL5420915 IC50 = 6.0 nM 8.22
CHEMBL5428866 IC50 = 9.0 nM 8.05
CHEMBL5440226 IC50 = 10.0 nM 8.00
CHEMBL5419715 IC50 = 10.0 nM 8.00
CHEMBL5438063 IC50 = 12.0 nM 7.92
CHEMBL5421527 IC50 = 14.0 nM 7.85
CHEMBL5409780 IC50 = 20.0 nM 7.70
CHEMBL5396123 IC50 = 21.0 nM 7.68
CHEMBL5423100 IC50 = 25.0 nM 7.60
CHEMBL5419691 IC50 = 25.0 nM 7.60
CHEMBL5411270 IC50 = 40.0 nM 7.40
CHEMBL5413258 IC50 = 43.0 nM 7.37
CHEMBL5409162 IC50 = 46.0 nM 7.34
CHEMBL5421587 IC50 = 47.0 nM 7.33
CHEMBL5440331 IC50 = 50.0 nM 7.30
CHEMBL5430225 IC50 = 55.0 nM 7.26
CHEMBL5419772 IC50 = 74.0 nM 7.13
CHEMBL5404877 IC50 = 79.0 nM 7.10
CHEMBL5439995 IC50 = 82.0 nM 7.09
CHEMBL5406720 IC50 = 92.0 nM 7.04
CHEMBL5405502 IC50 = 91.0 nM 7.04
CHEMBL5436706 IC50 = 95.0 nM 7.02
CHEMBL5425977 IC50 = 104.0 nM 6.98
CHEMBL5403832 IC50 = 106.0 nM 6.97
CHEMBL5424203 IC50 = 117.0 nM 6.93
CHEMBL5424511 IC50 = 155.0 nM 6.81
CHEMBL5438393 IC50 = 180.0 nM 6.75
CHEMBL5438750 IC50 = 183.0 nM 6.74
CHEMBL5421956 IC50 = 213.0 nM 6.67
CHEMBL5398523 IC50 = 216.0 nM 6.67
CHEMBL5416160 IC50 = 219.0 nM 6.66
CHEMBL5395908 IC50 = 335.0 nM 6.47
CHEMBL5395824 IC50 = 557.0 nM 6.25
CHEMBL5411384 IC50 = 576.0 nM 6.24
CHEMBL5414916 IC50 = 615.0 nM 6.21
CHEMBL5413604 IC50 = 1220.0 nM 5.91
CHEMBL5434011 IC50 = 2815.0 nM 5.55