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Assay Detail

CHEMBL658107

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Binding
Inhibitory activity against human CDK2 (Cyclin dependent kinase 2)
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cyclin-dependent kinase 2 (CHEMBL301)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.
Wang S, Meades C, Wood G, Osnowski A, Anderson S, Yuill R, Thomas M, Mezna M, Jackson W, Midgley C, Griffiths G, Fleming I, Green S, McNae I, Wu SY, McInnes C, Zheleva D, Walkinshaw MD, Fischer PM.
J Med Chem (2004) 47 : 1662 -1675
PubMed 15027857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.73 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298445 1 8.70
CHEMBL295484 1 7.70
CHEMBL431336 1 7.52
CHEMBL297412 1 7.40
CHEMBL46401 1 7.22
CHEMBL47527 1 7.22
CHEMBL47590 1 7.16
CHEMBL295127 1 7.10
CHEMBL432116 1 7.00
CHEMBL433068 1 7.00
CHEMBL45408 1 6.96
CHEMBL44119 1 6.96
CHEMBL442957 1 6.85
CHEMBL47249 1 6.80
CHEMBL46817 1 6.66
CHEMBL48109 1 6.54
CHEMBL47132 1 6.52
CHEMBL47636 1 6.40
CHEMBL44712 1 6.17
CHEMBL295398 1 6.16
CHEMBL46429 1 6.10
CHEMBL297447 1 5.92
CHEMBL45001 1 5.60
CHEMBL47690 1 5.39
CHEMBL47302 1 5.19
CHEMBL47276 1 -
CHEMBL43828 1 -
CHEMBL409506 1 -
CHEMBL48019 1 -
CHEMBL297614 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298445 Ki = 2.0 nM 8.70
CHEMBL295484 Ki = 20.0 nM 7.70
CHEMBL431336 Ki = 30.0 nM 7.52
CHEMBL297412 Ki = 40.0 nM 7.40
CHEMBL46401 Ki = 60.0 nM 7.22
CHEMBL47527 Ki = 60.0 nM 7.22
CHEMBL47590 Ki = 70.0 nM 7.16
CHEMBL295127 Ki = 80.0 nM 7.10
CHEMBL432116 Ki = 100.0 nM 7.00
CHEMBL433068 Ki = 100.0 nM 7.00
CHEMBL45408 Ki = 110.0 nM 6.96
CHEMBL44119 Ki = 110.0 nM 6.96
CHEMBL442957 Ki = 140.0 nM 6.85
CHEMBL47249 Ki = 160.0 nM 6.80
CHEMBL46817 Ki = 220.0 nM 6.66
CHEMBL48109 Ki = 290.0 nM 6.54
CHEMBL47132 Ki = 300.0 nM 6.52
CHEMBL47636 Ki = 400.0 nM 6.40
CHEMBL44712 Ki = 670.0 nM 6.17
CHEMBL295398 Ki = 700.0 nM 6.16
CHEMBL46429 Ki = 800.0 nM 6.10
CHEMBL297447 Ki = 1200.0 nM 5.92
CHEMBL45001 Ki = 2500.0 nM 5.60
CHEMBL47690 Ki = 4100.0 nM 5.39
CHEMBL47302 Ki = 6500.0 nM 5.19
CHEMBL47276 Ki > 20000.0 nM -
CHEMBL43828 Ki > 20000.0 nM -
CHEMBL409506 Ki > 20000.0 nM -
CHEMBL48019 Ki > 20000.0 nM -
CHEMBL297614 Ki > 20000.0 nM -
CHEMBL296666 Ki > 10000.0 nM -
CHEMBL44063 Ki > 20000.0 nM -
CHEMBL46474 Ki > 20000.0 nM -