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Assay Detail

CHEMBL4029487

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Binding
Inhibition of CDK8 (unknown origin) assessed as reduction in RNAP2 C-terminal domain phosphorylation
1
Total Activities
1
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 8 (CHEMBL5719)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.
Ono K, Banno H, Okaniwa M, Hirayama T, Iwamura N, Hikichi Y, Murai S, Hasegawa M, Hasegawa Y, Yonemori K, Hata A, Aoyama K, Cary DR.
Bioorg Med Chem (2017) 25 : 2336 -2350
PubMed 28302507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.92 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4080906 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4080906 IC50 = 12.0 nM 7.92