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Assay Detail

CHEMBL833553

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

Binding
Inhibition of cyclin dependent kinase 2-cyclin A
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin A (CHEMBL2094128)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.
Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C.
J Med Chem (2005) 48 : 2944 -2956
PubMed 15828833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.91 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190446 1 8.70
CHEMBL192602 1 8.70
CHEMBL193210 1 7.96
CHEMBL192716 1 7.92
CHEMBL370724 1 7.89
CHEMBL366032 1 7.89
CHEMBL192042 1 7.77
CHEMBL193288 1 7.77
CHEMBL191834 1 7.70
CHEMBL192556 1 7.70
CHEMBL192339 1 7.60
CHEMBL359556 1 7.54
CHEMBL115220 1 7.43
CHEMBL191144 1 7.43
CHEMBL370817 1 7.14
CHEMBL373346 1 7.11
CHEMBL365341 1 7.10
CHEMBL366230 1 7.08
CHEMBL191733 1 7.00
CHEMBL372467 1 6.91
CHEMBL193673 1 6.82
CHEMBL192126 1 6.77
CHEMBL195683 1 6.77
CHEMBL193622 1 6.77
CHEMBL192440 1 6.70
CHEMBL190206 1 6.70
CHEMBL191865 1 6.62
CHEMBL189047 1 6.34
CHEMBL193287 1 6.02
CHEMBL191948 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190446 IC50 = 2.0 nM 8.70
CHEMBL192602 IC50 = 2.0 nM 8.70
CHEMBL193210 IC50 = 11.0 nM 7.96
CHEMBL192716 IC50 = 12.0 nM 7.92
CHEMBL370724 IC50 = 13.0 nM 7.89
CHEMBL366032 IC50 = 13.0 nM 7.89
CHEMBL192042 IC50 = 17.0 nM 7.77
CHEMBL193288 IC50 = 17.0 nM 7.77
CHEMBL191834 IC50 = 20.0 nM 7.70
CHEMBL192556 IC50 = 20.0 nM 7.70
CHEMBL192339 IC50 = 25.0 nM 7.60
CHEMBL359556 IC50 = 29.0 nM 7.54
CHEMBL115220 IC50 = 37.0 nM 7.43
CHEMBL191144 IC50 = 37.0 nM 7.43
CHEMBL370817 IC50 = 73.0 nM 7.14
CHEMBL373346 IC50 = 77.0 nM 7.11
CHEMBL365341 IC50 = 80.0 nM 7.10
CHEMBL366230 IC50 = 84.0 nM 7.08
CHEMBL191733 IC50 = 99.0 nM 7.00
CHEMBL372467 IC50 = 124.0 nM 6.91
CHEMBL193673 IC50 = 150.0 nM 6.82
CHEMBL192126 IC50 = 170.0 nM 6.77
CHEMBL195683 IC50 = 169.0 nM 6.77
CHEMBL193622 IC50 = 169.0 nM 6.77
CHEMBL192440 IC50 = 200.0 nM 6.70
CHEMBL190206 IC50 = 200.0 nM 6.70
CHEMBL191865 IC50 = 240.0 nM 6.62
CHEMBL189047 IC50 = 455.0 nM 6.34
CHEMBL193287 IC50 = 960.0 nM 6.02
CHEMBL191948 IC50 = 1450.0 nM 5.84
CHEMBL190154 IC50 = 2000.0 nM 5.70
CHEMBL192471 IC50 = 2500.0 nM 5.60
CHEMBL192179 IC50 = 2500.0 nM 5.60
CHEMBL190178 IC50 = 2600.0 nM 5.58
CHEMBL189791 IC50 = 5000.0 nM 5.30
CHEMBL365988 IC50 = 6000.0 nM 5.22
CHEMBL365355 IC50 = 8500.0 nM 5.07
CHEMBL370036 IC50 > 10000.0 nM -
CHEMBL192665 IC50 > 10000.0 nM -