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Assay Detail

CHEMBL5166985

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

Binding
Inhibition of recombinant full length His tagged human CDK8/Cyclin C expressed in Baculovirus incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
34
Total Activities
34
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

CDK8/Cyclin C (CHEMBL3038474)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease <i>In Vivo</i>.
Yan Y, Xing C, Xiao Y, Shen X, Zhang Z, He C, Shi JB, Liu M, Liu X.
J Med Chem (2022) 65 : 7334 -7362
PubMed 35536548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.63 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5199685 1 7.25
CHEMBL5197084 1 7.19
CHEMBL5185339 1 7.16
CHEMBL5176173 1 7.14
CHEMBL5194157 1 7.12
CHEMBL5182399 1 7.10
CHEMBL5178431 1 7.10
CHEMBL5190284 1 7.09
CHEMBL5174097 1 7.06
CHEMBL5177563 1 7.02
CHEMBL5209397 1 6.98
CHEMBL5206315 1 6.95
CHEMBL5195098 1 6.87
CHEMBL5194000 1 6.87
CHEMBL5208801 1 6.84
CHEMBL5169782 1 6.81
CHEMBL5175354 1 6.79
CHEMBL5188393 1 6.75
CHEMBL5180489 1 6.72
CHEMBL5188999 1 6.69
CHEMBL1409113 1 6.68
CHEMBL5196466 1 6.68
CHEMBL5174635 1 6.67
CHEMBL5196442 1 6.63
CHEMBL5181302 1 6.58
CHEMBL5198747 1 6.28
CHEMBL5181742 1 6.26
CHEMBL5175136 1 6.02
CHEMBL5193697 1 5.98
CHEMBL5177445 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5199685 IC50 = 56.0 nM 7.25
CHEMBL5197084 IC50 = 65.0 nM 7.19
CHEMBL5185339 IC50 = 70.0 nM 7.16
CHEMBL5176173 IC50 = 72.0 nM 7.14
CHEMBL5194157 IC50 = 75.0 nM 7.12
CHEMBL5182399 IC50 = 80.0 nM 7.10
CHEMBL5178431 IC50 = 80.0 nM 7.10
CHEMBL5190284 IC50 = 81.0 nM 7.09
CHEMBL5174097 IC50 = 87.0 nM 7.06
CHEMBL5177563 IC50 = 96.0 nM 7.02
CHEMBL5209397 IC50 = 104.0 nM 6.98
CHEMBL5206315 IC50 = 112.0 nM 6.95
CHEMBL5195098 IC50 = 134.0 nM 6.87
CHEMBL5194000 IC50 = 134.0 nM 6.87
CHEMBL5208801 IC50 = 144.0 nM 6.84
CHEMBL5169782 IC50 = 155.0 nM 6.81
CHEMBL5175354 IC50 = 162.0 nM 6.79
CHEMBL5188393 IC50 = 177.0 nM 6.75
CHEMBL5180489 IC50 = 190.0 nM 6.72
CHEMBL5188999 IC50 = 205.0 nM 6.69
CHEMBL1409113 IC50 = 211.0 nM 6.68
CHEMBL5196466 IC50 = 210.0 nM 6.68
CHEMBL5174635 IC50 = 214.0 nM 6.67
CHEMBL5196442 IC50 = 234.0 nM 6.63
CHEMBL5181302 IC50 = 260.0 nM 6.58
CHEMBL5198747 IC50 = 530.0 nM 6.28
CHEMBL5181742 IC50 = 548.0 nM 6.26
CHEMBL5175136 IC50 = 947.0 nM 6.02
CHEMBL5193697 IC50 = 1050.0 nM 5.98
CHEMBL5177445 IC50 = 1140.0 nM 5.94
CHEMBL5188825 IC50 = 1470.0 nM 5.83
CHEMBL5194811 IC50 = 2110.0 nM 5.68
CHEMBL5179301 IC50 = 3654.0 nM 5.44
CHEMBL16171 WOGONIN IC50 = 5900.0 nM 5.23