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Assay Detail

CHEMBL622591

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Functional
Antiproliferative activity against human A2780 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Expert

Target

A2780 (CHEMBL614004)
Type CELL-LINE
Organism Homo sapiens

Publication

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.
Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA.
J Med Chem (2004) 47 : 3367 -3380
PubMed 15189033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.14 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115933 1 6.96
CHEMBL114636 1 6.92
CHEMBL114718 1 6.74
CHEMBL114790 1 6.69
CHEMBL115220 1 6.54
CHEMBL326501 1 6.05
CHEMBL114851 1 5.85
CHEMBL112433 1 5.83
CHEMBL324577 1 5.55
CHEMBL115994 1 5.30
CHEMBL323821 1 5.16
CHEMBL114917 1 -
CHEMBL114156 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115933 IC50 = 111.0 nM 6.96
CHEMBL114636 IC50 = 121.0 nM 6.92
CHEMBL114718 IC50 = 182.0 nM 6.74
CHEMBL114790 IC50 = 205.0 nM 6.69
CHEMBL115220 IC50 = 286.0 nM 6.54
CHEMBL326501 IC50 = 900.0 nM 6.05
CHEMBL114851 IC50 = 1400.0 nM 5.85
CHEMBL112433 IC50 = 1468.0 nM 5.83
CHEMBL324577 IC50 = 2835.0 nM 5.55
CHEMBL115994 IC50 = 4990.0 nM 5.30
CHEMBL323821 IC50 = 6984.0 nM 5.16
CHEMBL114917 IC50 > 20000.0 nM -
CHEMBL114156 IC50 > 20000.0 nM -