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Assay Detail

CHEMBL992478

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

Binding
Inhibition of CDK2
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.
Anderson M, Andrews DM, Barker AJ, Brassington CA, Breed J, Byth KF, Culshaw JD, Finlay MR, Fisher E, McMiken HH, Green CP, Heaton DW, Nash IA, Newcombe NJ, Oakes SE, Pauptit RA, Roberts A, Stanway JJ, Thomas AP, Tucker JA, Walker M, Weir HM.
Bioorg Med Chem Lett (2008) 18 : 5487 -5492
PubMed 18815031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.78 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478409 1 9.00
CHEMBL73303 1 8.70
CHEMBL485618 1 8.40
CHEMBL488436 AZD-5438 1.0 1 8.22
CHEMBL520353 1 8.22
CHEMBL485240 1 8.10
CHEMBL484571 1 8.10
CHEMBL520187 1 8.10
CHEMBL484738 1 7.96
CHEMBL515839 1 7.89
CHEMBL515854 1 7.85
CHEMBL485619 1 7.82
CHEMBL457979 1 7.72
CHEMBL514913 1 7.64
CHEMBL485431 1 7.60
CHEMBL457888 1 7.48
CHEMBL457887 1 7.44
CHEMBL458547 1 7.17
CHEMBL483590 1 7.08
CHEMBL458548 1 6.53
CHEMBL485602 1 6.40
CHEMBL484555 1 -
CHEMBL485425 1 -
CHEMBL520003 1 -
CHEMBL309573 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478409 IC50 = 1.0 nM 9.00
CHEMBL73303 IC50 = 2.0 nM 8.70
CHEMBL485618 IC50 = 4.0 nM 8.40
CHEMBL488436 AZD-5438 IC50 = 6.0 nM 8.22
CHEMBL520353 IC50 = 6.0 nM 8.22
CHEMBL485240 IC50 = 8.0 nM 8.10
CHEMBL484571 IC50 = 8.0 nM 8.10
CHEMBL520187 IC50 = 8.0 nM 8.10
CHEMBL484738 IC50 = 11.0 nM 7.96
CHEMBL515839 IC50 = 13.0 nM 7.89
CHEMBL515854 IC50 = 14.0 nM 7.85
CHEMBL485619 IC50 = 15.0 nM 7.82
CHEMBL457979 IC50 = 19.0 nM 7.72
CHEMBL514913 IC50 = 23.0 nM 7.64
CHEMBL485431 IC50 = 25.0 nM 7.60
CHEMBL457888 IC50 = 33.0 nM 7.48
CHEMBL457887 IC50 = 36.0 nM 7.44
CHEMBL458547 IC50 = 68.0 nM 7.17
CHEMBL483590 IC50 = 83.0 nM 7.08
CHEMBL458548 IC50 = 295.0 nM 6.53
CHEMBL485602 IC50 = 400.0 nM 6.40
CHEMBL484555 IC50 < 3.0 nM -
CHEMBL485425 IC50 < 3.0 nM -
CHEMBL520003 IC50 < 3.0 nM -
CHEMBL309573 IC50 < 12.0 nM -