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Assay Detail

CHEMBL5504167

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Binding
Inhibition of CDK9 (unknown origin) using ULight 4EBP1 peptide as substrate incubated for 1 hr in presence of ATP by FRET assay
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 9 (CHEMBL3116) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Orally Bioavailable and Potent CDK9 Inhibitors for Targeting Transcription Regulation in Triple-Negative Breast Cancer.
Wang WJ, Gao L, Wang S, Huang W, Meng XY, Hu H, Chen Z, Sun J, Yuan Y, Zhou Y, Diao X, Huang R, Li J, Chen XH.
J Med Chem (2024) 67 : 10035 -10056
PubMed 38885173 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.98 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5537078 — — 1 8.06
CHEMBL5532236 — — 1 8.00
CHEMBL2103840 DINACICLIB 3.0 1 7.97
CHEMBL5532052 — — 1 7.88
CHEMBL5555666 — — 1 7.82
CHEMBL5556871 — — 1 7.82
CHEMBL5558477 — — 1 7.77
CHEMBL5557963 — — 1 7.76
CHEMBL5542666 — — 1 7.74
CHEMBL5512555 — — 1 7.63
CHEMBL5537062 — — 1 7.61
CHEMBL5505838 — — 1 7.59
CHEMBL5527848 — — 1 7.55
CHEMBL5555640 — — 1 7.54
CHEMBL5555057 — — 1 7.53
CHEMBL5542924 — — 1 7.53
CHEMBL5532122 — — 1 7.52
CHEMBL5505818 — — 1 7.50
CHEMBL5542804 — — 1 7.45
CHEMBL5505745 — — 1 7.43
CHEMBL5517681 — — 1 7.37
CHEMBL5531956 — — 1 7.35
CHEMBL5555560 — — 1 7.34
CHEMBL5527858 — — 1 7.14
CHEMBL5559108 — — 1 7.11
CHEMBL5558295 — — 1 7.05
CHEMBL5559473 — — 1 7.02
CHEMBL5542488 — — 1 6.99
CHEMBL5517691 — — 1 6.98
CHEMBL5518081 — — 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5537078 — IC50 = 8.7 nM 8.06
CHEMBL5532236 — IC50 = 9.99 nM 8.00
CHEMBL2103840 DINACICLIB IC50 = 10.64 nM 7.97
CHEMBL5532052 — IC50 = 13.06 nM 7.88
CHEMBL5555666 — IC50 = 15.05 nM 7.82
CHEMBL5556871 — IC50 = 15.17 nM 7.82
CHEMBL5558477 — IC50 = 16.91 nM 7.77
CHEMBL5557963 — IC50 = 17.44 nM 7.76
CHEMBL5542666 — IC50 = 18.23 nM 7.74
CHEMBL5512555 — IC50 = 23.53 nM 7.63
CHEMBL5537062 — IC50 = 24.65 nM 7.61
CHEMBL5505838 — IC50 = 25.47 nM 7.59
CHEMBL5527848 — IC50 = 28.01 nM 7.55
CHEMBL5555640 — IC50 = 28.9 nM 7.54
CHEMBL5542924 — IC50 = 29.66 nM 7.53
CHEMBL5555057 — IC50 = 29.85 nM 7.53
CHEMBL5532122 — IC50 = 30.17 nM 7.52
CHEMBL5505818 — IC50 = 31.51 nM 7.50
CHEMBL5542804 — IC50 = 35.38 nM 7.45
CHEMBL5505745 — IC50 = 37.34 nM 7.43
CHEMBL5517681 — IC50 = 43.2 nM 7.37
CHEMBL5531956 — IC50 = 44.82 nM 7.35
CHEMBL5555560 — IC50 = 45.68 nM 7.34
CHEMBL5527858 — IC50 = 72.67 nM 7.14
CHEMBL5559108 — IC50 = 77.01 nM 7.11
CHEMBL5558295 — IC50 = 88.03 nM 7.05
CHEMBL5559473 — IC50 = 95.01 nM 7.02
CHEMBL5542488 — IC50 = 101.41 nM 6.99
CHEMBL5517691 — IC50 = 103.99 nM 6.98
CHEMBL5518081 — IC50 = 129.4 nM 6.89
CHEMBL5512517 — IC50 = 129.65 nM 6.89
CHEMBL5542710 — IC50 = 150.15 nM 6.82
CHEMBL5542095 — IC50 = 250.3 nM 6.60
CHEMBL5559020 — IC50 = 268.0 nM 6.57
CHEMBL5558604 — IC50 = 375.4 nM 6.43
CHEMBL4849464 — IC50 = 1071.9 nM 5.97
CHEMBL5517798 — IC50 = 1296.5 nM 5.89
CHEMBL5558916 — IC50 = 1905.0 nM 5.72
CHEMBL5512494 — IC50 = 2545.0 nM 5.59
CHEMBL5555405 — IC50 = 3736.5 nM 5.43
CHEMBL5556362 — IC50 = 4475.5 nM 5.35
CHEMBL5556898 — IC50 = 5703.0 nM 5.24
CHEMBL5556499 — IC50 = 11621.0 nM 4.93
CHEMBL5557269 — IC50 = 14461.0 nM 4.84
CHEMBL5555502 — IC50 > 20000.0 nM -
CHEMBL5559007 — IC50 > 20000.0 nM -
CHEMBL5523441 — IC50 > 20000.0 nM -
CHEMBL5549863 — IC50 > 20000.0 nM -
CHEMBL5512510 — IC50 > 20000.0 nM -