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Assay Detail

CHEMBL3624762

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Functional
Antiproliferative activity against human MCF7 cells
18
Total Activities
18
Compounds Tested
2
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

Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
De Savi C, Bradbury RH, Rabow AA, Norman RA, de Almeida C, Andrews DM, Ballard P, Buttar D, Callis RJ, Currie GS, Curwen JO, Davies CD, Donald CS, Feron LJ, Gingell H, Glossop SC, Hayter BR, Hussain S, Karoutchi G, Lamont SG, MacFaul P, Moss TA, Pearson SE, Tonge M, Walker GE, Weir HM, Wilson Z.
J Med Chem (2015) 58 : 8128 -8140
PubMed 26407012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.21 10.40
pIC50 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3623004 AZD-9496 1.0 1 10.40
CHEMBL1358 FULVESTRANT 4.0 1 10.00
CHEMBL3623002 1 9.64
CHEMBL3623003 1 9.49
CHEMBL2137046 1 9.27
CHEMBL3623001 1 9.11
CHEMBL3622999 1 7.65
CHEMBL83 TAMOXIFEN 4.0 1 7.24
CHEMBL33899 1 6.53
CHEMBL3622998 1 6.09
CHEMBL3622994 1 4.86
CHEMBL3622996 1 -
CHEMBL3622995 1 -
CHEMBL3622993 1 -
CHEMBL3622992 1 -
CHEMBL195515 1 -
CHEMBL3622997 1 -
CHEMBL3623000 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3623004 AZD-9496 IC50 = 0.03981 nM 10.40
CHEMBL1358 FULVESTRANT IC50 = 0.1 nM 10.00
CHEMBL3623002 IC50 = 0.2291 nM 9.64
CHEMBL3623003 IC50 = 0.3236 nM 9.49
CHEMBL2137046 IC50 = 0.537 nM 9.27
CHEMBL3623001 IC50 = 0.7762 nM 9.11
CHEMBL3622999 IC50 = 22.39 nM 7.65
CHEMBL83 TAMOXIFEN IC50 = 57.54 nM 7.24
CHEMBL33899 IC50 = 295.12 nM 6.53
CHEMBL3622998 IC50 = 812.83 nM 6.09
CHEMBL3622994 IC50 = 13803.84 nM 4.86
CHEMBL3622996 IC50 > 31622.78 nM -
CHEMBL3622995 IC50 > 25118.86 nM -
CHEMBL3622993 pIC50 - -
CHEMBL3622992 pIC50 - -
CHEMBL195515 pIC50 - -
CHEMBL3622997 IC50 > 31622.78 nM -
CHEMBL3623000 pIC50 - -