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Assay Detail

CHEMBL5336209

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

Binding
Inhibition of CDK12/Cyclin K (unknown origin) preincubated for 10 mins followed by substrate and ATP addition measured after 200 mins by ADP-Glo luminescence assay
10
Total Activities
10
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

CDK12/Cyclin K (CHEMBL4106169)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Development, validation, and evaluation of a deep learning model to screen cyclin-dependent kinase 12 inhibitors in cancers.
Wen T, Wang J, Lu R, Tan S, Li P, Yao X, Liu H, Yi Z, Li L, Liu S, Gao P, Qian H, Xie G, Ma F.
Eur J Med Chem (2023) 250 : 115199 -115199
PubMed 36827953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.64 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4632717 1 7.28
CHEMBL4468670 1 7.13
CHEMBL6291 BISINDOLYLMALEIMIDE IX 1 6.84
CHEMBL4163879 1 6.82
CHEMBL4077071 1 6.74
CHEMBL5420867 1 6.58
CHEMBL4762845 1 6.37
CHEMBL468963 GW779439X 1 6.36
CHEMBL3672295 1 6.14
CHEMBL5420897 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4632717 IC50 = 52.97 nM 7.28
CHEMBL4468670 IC50 = 74.39 nM 7.13
CHEMBL6291 BISINDOLYLMALEIMIDE IX IC50 = 143.1 nM 6.84
CHEMBL4163879 IC50 = 152.1 nM 6.82
CHEMBL4077071 IC50 = 183.5 nM 6.74
CHEMBL5420867 IC50 = 260.4 nM 6.58
CHEMBL4762845 IC50 = 425.4 nM 6.37
CHEMBL468963 GW779439X IC50 = 435.0 nM 6.36
CHEMBL3672295 IC50 = 726.7 nM 6.14
CHEMBL5420897 IC50 = 748.9 nM 6.13