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Assay Detail

CHEMBL4612776

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

Binding
Inhibition of human CDK12/cyclin K using Pol2-CTD as substrate by [gamma-33P]ATP-based radioisotope filter binding assay
1
Total Activities
1
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

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
Liu Y, Hao M, Leggett AL, Gao Y, Ficarro SB, Che J, He Z, Olson CM, Marto JA, Kwiatkowski NP, Zhang T, Gray NS.
J Med Chem (2020) 63 : 6708 -6726
PubMed 32502343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.60 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4647764 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4647764 IC50 = 25.0 nM 7.60