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Assay Detail

CHEMBL5115861

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

Binding
Inhibition of human recombinant full length GST-tagged CDK6/Cyclin D1 expressed in Baculovirus expression system by Adapta assay
31
Total Activities
31
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

CDK6/cyclin D1 (CHEMBL2111455)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold.
Li Z, Ishida R, Liu Y, Wang J, Li Y, Gao Y, Jiang J, Che J, Sheltzer JM, Robers MB, Zhang T, Westover KD, Nabet B, Gray NS.
Eur J Med Chem (2022) 238 : 114433 -114433
PubMed 35597007 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.71 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1989043 1 8.40
CHEMBL5206282 1 7.77
CHEMBL5185655 1 7.75
CHEMBL5171843 1 7.68
CHEMBL5184522 1 7.54
CHEMBL5185990 1 7.50
CHEMBL5175800 1 7.47
CHEMBL5200963 1 7.42
CHEMBL5178437 1 7.21
CHEMBL5170651 1 6.81
CHEMBL5182610 1 6.78
CHEMBL5180190 1 6.66
CHEMBL5180130 1 6.57
CHEMBL5169674 1 6.46
CHEMBL5180851 1 6.34
CHEMBL5173236 1 6.30
CHEMBL5190514 1 6.23
CHEMBL5200515 1 6.19
CHEMBL5194816 1 6.17
CHEMBL5208491 1 6.12
CHEMBL5203750 1 6.09
CHEMBL5190264 1 6.05
CHEMBL5200790 1 6.04
CHEMBL5177982 1 6.04
CHEMBL5189171 1 6.01
CHEMBL5180577 1 5.85
CHEMBL5199067 1 5.81
CHEMBL5173735 1 -
CHEMBL5195298 1 -
CHEMBL5207135 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1989043 IC50 = 4.0 nM 8.40
CHEMBL5206282 IC50 = 17.0 nM 7.77
CHEMBL5185655 IC50 = 18.0 nM 7.75
CHEMBL5171843 IC50 = 21.0 nM 7.68
CHEMBL5184522 IC50 = 29.0 nM 7.54
CHEMBL5185990 IC50 = 32.0 nM 7.50
CHEMBL5175800 IC50 = 34.0 nM 7.47
CHEMBL5200963 IC50 = 38.0 nM 7.42
CHEMBL5178437 IC50 = 61.0 nM 7.21
CHEMBL5170651 IC50 = 156.0 nM 6.81
CHEMBL5182610 IC50 = 166.0 nM 6.78
CHEMBL5180190 IC50 = 217.0 nM 6.66
CHEMBL5180130 IC50 = 272.0 nM 6.57
CHEMBL5169674 IC50 = 348.0 nM 6.46
CHEMBL5180851 IC50 = 455.0 nM 6.34
CHEMBL5173236 IC50 = 498.0 nM 6.30
CHEMBL5190514 IC50 = 593.0 nM 6.23
CHEMBL5200515 IC50 = 652.0 nM 6.19
CHEMBL5194816 IC50 = 677.0 nM 6.17
CHEMBL5208491 IC50 = 758.0 nM 6.12
CHEMBL5203750 IC50 = 805.0 nM 6.09
CHEMBL5190264 IC50 = 886.0 nM 6.05
CHEMBL5200790 IC50 = 914.0 nM 6.04
CHEMBL5177982 IC50 = 918.0 nM 6.04
CHEMBL5189171 IC50 = 985.0 nM 6.01
CHEMBL5180577 IC50 = 1410.0 nM 5.85
CHEMBL5199067 IC50 = 1540.0 nM 5.81
CHEMBL5173735 IC50 > 10000.0 nM -
CHEMBL5195298 IC50 > 10000.0 nM -
CHEMBL5207135 IC50 > 10000.0 nM -
CHEMBL5192162 IC50 > 10000.0 nM -