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Assay Detail

CHEMBL1016203

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

Functional
Cytotoxicity against human MCF7 cells after 3 days by SRB assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Autocuration

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.
Tsou HR, Liu X, Birnberg G, Kaplan J, Otteng M, Tran T, Kutterer K, Tang Z, Suayan R, Zask A, Ravi M, Bretz A, Grillo M, McGinnis JP, Rabindran SK, Ayral-Kaloustian S, Mansour TS.
J Med Chem (2009) 52 : 2289 -2310
PubMed 19317452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.93 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477259 1 6.52
CHEMBL451298 1 6.27
CHEMBL477877 1 6.16
CHEMBL514678 1 6.16
CHEMBL515631 1 6.16
CHEMBL490240 1 6.08
CHEMBL478488 1 6.06
CHEMBL477064 1 6.06
CHEMBL477063 1 6.00
CHEMBL452447 1 5.96
CHEMBL504547 1 5.95
CHEMBL477863 1 5.85
CHEMBL489629 1 5.85
CHEMBL477860 1 5.82
CHEMBL477861 1 5.75
CHEMBL521922 1 5.57
CHEMBL489245 1 5.43
CHEMBL478487 1 5.09
CHEMBL477862 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477259 IC50 = 300.0 nM 6.52
CHEMBL451298 IC50 = 540.0 nM 6.27
CHEMBL477877 IC50 = 700.0 nM 6.16
CHEMBL514678 IC50 = 700.0 nM 6.16
CHEMBL515631 IC50 = 700.0 nM 6.16
CHEMBL490240 IC50 = 830.0 nM 6.08
CHEMBL478488 IC50 = 880.0 nM 6.06
CHEMBL477064 IC50 = 880.0 nM 6.06
CHEMBL477063 IC50 = 1000.0 nM 6.00
CHEMBL452447 IC50 = 1100.0 nM 5.96
CHEMBL504547 IC50 = 1130.0 nM 5.95
CHEMBL477863 IC50 = 1400.0 nM 5.85
CHEMBL489629 IC50 = 1400.0 nM 5.85
CHEMBL477860 IC50 = 1500.0 nM 5.82
CHEMBL477861 IC50 = 1800.0 nM 5.75
CHEMBL521922 IC50 = 2700.0 nM 5.57
CHEMBL489245 IC50 = 3700.0 nM 5.43
CHEMBL478487 IC50 = 8200.0 nM 5.09
CHEMBL477862 IC50 > 50000.0 nM -