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Assay Detail

CHEMBL622593

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Functional
Antiproliferative effect against human A2780 cell line was determined in a whole cell 72 hr cytotoxicity assay
17
Total Activities
17
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

N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.
Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ, Qian L, Chen BC, Zhao R, Bednarz MS, Kellar KA, Mulheron JG, Batorsky R, Roongta U, Kamath A, Marathe P, Ranadive SA, Sack JS, Tokarski JS, Pavletich NP, Lee FY, Webster KR, Kimball SD.
J Med Chem (2004) 47 : 1719 -1728
PubMed 15027863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.75 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300936 1 7.54
CHEMBL297755 1 7.54
CHEMBL49618 1 7.31
CHEMBL295136 1 7.30
CHEMBL428690 ALVOCIDIB 3.0 1 7.15
CHEMBL301316 1 7.11
CHEMBL296468 BMS-387032 1.0 1 7.02
CHEMBL45860 1 7.00
CHEMBL45757 1 6.96
CHEMBL49814 1 6.92
CHEMBL297570 1 6.75
CHEMBL47116 1 6.75
CHEMBL301184 1 6.28
CHEMBL48796 1 6.08
CHEMBL46164 1 5.80
CHEMBL295835 1 5.75
CHEMBL295918 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300936 IC50 = 29.0 nM 7.54
CHEMBL297755 IC50 = 29.0 nM 7.54
CHEMBL49618 IC50 = 49.0 nM 7.31
CHEMBL295136 IC50 = 50.0 nM 7.30
CHEMBL428690 ALVOCIDIB IC50 = 71.0 nM 7.15
CHEMBL301316 IC50 = 78.0 nM 7.11
CHEMBL296468 BMS-387032 IC50 = 95.0 nM 7.02
CHEMBL45860 IC50 = 100.0 nM 7.00
CHEMBL45757 IC50 = 110.0 nM 6.96
CHEMBL49814 IC50 = 120.0 nM 6.92
CHEMBL297570 IC50 = 180.0 nM 6.75
CHEMBL47116 IC50 = 180.0 nM 6.75
CHEMBL301184 IC50 = 520.0 nM 6.28
CHEMBL48796 IC50 = 840.0 nM 6.08
CHEMBL46164 IC50 = 1600.0 nM 5.80
CHEMBL295835 IC50 = 1800.0 nM 5.75
CHEMBL295918 IC50 = 2900.0 nM 5.54