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Assay Detail

CHEMBL1064459

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Functional
Antiproliferative activity against human A2780 cells after 72 hrs by fluorescence assay
ChEMBL ↗
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

A2780 (CHEMBL614004) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M.
Bioorg Med Chem (2010) 18 : 1844 -1853
PubMed 20153204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.61 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1744452 — — 1 7.52
CHEMBL603249 — — 1 7.22
CHEMBL1744450 — — 1 7.22
CHEMBL1230607 PHA-793887 1.0 1 7.05
CHEMBL603478 — — 1 7.00
CHEMBL606412 — — 1 6.96
CHEMBL599237 — — 1 6.92
CHEMBL598221 — — 1 6.92
CHEMBL603887 — — 1 6.89
CHEMBL1744453 — — 1 6.85
CHEMBL1744456 — — 1 6.85
CHEMBL606336 — — 1 6.80
CHEMBL597199 — — 1 6.75
CHEMBL599249 — — 1 6.70
CHEMBL597390 — — 1 6.57
CHEMBL1744449 — — 1 6.57
CHEMBL603543 — — 1 6.54
CHEMBL604712 — — 1 6.51
CHEMBL1744458 — — 1 6.50
CHEMBL596978 — — 1 6.46
CHEMBL599033 — — 1 6.46
CHEMBL605327 — — 1 6.42
CHEMBL1744457 — — 1 6.39
CHEMBL1744451 — — 1 6.30
CHEMBL599034 — — 1 6.24
CHEMBL606187 — — 1 6.19
CHEMBL591898 — — 1 6.19
CHEMBL603243 — — 1 6.19
CHEMBL597391 — — 1 6.16
CHEMBL1744455 — — 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1744452 — IC50 = 30.0 nM 7.52
CHEMBL603249 — IC50 = 60.0 nM 7.22
CHEMBL1744450 — IC50 = 60.0 nM 7.22
CHEMBL1230607 PHA-793887 IC50 = 90.0 nM 7.05
CHEMBL603478 — IC50 = 100.0 nM 7.00
CHEMBL606412 — IC50 = 110.0 nM 6.96
CHEMBL599237 — IC50 = 120.0 nM 6.92
CHEMBL598221 — IC50 = 120.0 nM 6.92
CHEMBL603887 — IC50 = 130.0 nM 6.89
CHEMBL1744456 — IC50 = 140.0 nM 6.85
CHEMBL1744453 — IC50 = 140.0 nM 6.85
CHEMBL606336 — IC50 = 160.0 nM 6.80
CHEMBL597199 — IC50 = 180.0 nM 6.75
CHEMBL599249 — IC50 = 200.0 nM 6.70
CHEMBL1744449 — IC50 = 270.0 nM 6.57
CHEMBL597390 — IC50 = 270.0 nM 6.57
CHEMBL603543 — IC50 = 290.0 nM 6.54
CHEMBL604712 — IC50 = 310.0 nM 6.51
CHEMBL1744458 — IC50 = 320.0 nM 6.50
CHEMBL599033 — IC50 = 350.0 nM 6.46
CHEMBL596978 — IC50 = 350.0 nM 6.46
CHEMBL605327 — IC50 = 380.0 nM 6.42
CHEMBL1744457 — IC50 = 410.0 nM 6.39
CHEMBL1744451 — IC50 = 500.0 nM 6.30
CHEMBL599034 — IC50 = 580.0 nM 6.24
CHEMBL603243 — IC50 = 650.0 nM 6.19
CHEMBL591898 — IC50 = 650.0 nM 6.19
CHEMBL606187 — IC50 = 650.0 nM 6.19
CHEMBL597391 — IC50 = 690.0 nM 6.16
CHEMBL1744455 — IC50 = 1420.0 nM 5.85
CHEMBL597992 — IC50 = 2680.0 nM 5.57
CHEMBL599657 — IC50 > 10000.0 nM -
CHEMBL604714 — IC50 > 5000.0 nM -
CHEMBL597198 — IC50 > 10000.0 nM -
CHEMBL603264 — IC50 - — -
CHEMBL1744454 — IC50 > 5000.0 nM -