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Assay Detail

CHEMBL889117

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Functional
Inhibition of estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation
34
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ishikawa (CHEMBL614649)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.
Richardson TI, Frank SA, Wang M, Clarke CA, Jones SA, Ying BP, Kohlman DT, Wallace OB, Shepherd TA, Dally RD, Palkowitz AD, Geiser AG, Bryant HU, Henck JW, Cohen IR, Rudmann DG, McCann DJ, Coutant DE, Oldham SW, Hummel CW, Fong KC, Hinklin R, Lewis G, Tian H, Dodge JA.
Bioorg Med Chem Lett (2007) 17 : 3544 -3549
PubMed 17482463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.15 8.68
Efficacy 17 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390020 2 8.68
CHEMBL243571 2 8.55
CHEMBL244205 2 8.49
CHEMBL244206 2 8.41
CHEMBL244000 2 8.33
CHEMBL390021 2 8.32
CHEMBL243791 2 8.31
CHEMBL243790 2 8.21
CHEMBL244001 2 8.17
CHEMBL244207 2 8.14
CHEMBL390448 2 8.10
CHEMBL243789 2 7.97
CHEMBL395291 2 7.84
CHEMBL428926 2 7.80
CHEMBL243970 2 7.79
CHEMBL243999 2 7.73
CHEMBL389907 2 7.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390020 IC50 = 2.1 nM 8.68
CHEMBL243571 IC50 = 2.8 nM 8.55
CHEMBL244205 IC50 = 3.2 nM 8.49
CHEMBL244206 IC50 = 3.9 nM 8.41
CHEMBL244000 IC50 = 4.7 nM 8.33
CHEMBL390021 IC50 = 4.8 nM 8.32
CHEMBL243791 IC50 = 4.9 nM 8.31
CHEMBL243790 IC50 = 6.1 nM 8.21
CHEMBL244001 IC50 = 6.7 nM 8.17
CHEMBL244207 IC50 = 7.2 nM 8.14
CHEMBL390448 IC50 = 8.0 nM 8.10
CHEMBL243789 IC50 = 10.7 nM 7.97
CHEMBL395291 IC50 = 14.5 nM 7.84
CHEMBL428926 IC50 = 15.7 nM 7.80
CHEMBL243970 IC50 = 16.2 nM 7.79
CHEMBL243999 IC50 = 18.5 nM 7.73
CHEMBL389907 IC50 = 22.2 nM 7.65
CHEMBL243571 Efficacy = 99.0 % -
CHEMBL390448 Efficacy = 99.0 % -
CHEMBL428926 Efficacy = 93.0 % -
CHEMBL244207 Efficacy = 98.0 % -
CHEMBL244206 Efficacy = 96.0 % -
CHEMBL390021 Efficacy = 97.0 % -
CHEMBL244205 Efficacy = 93.0 % -
CHEMBL244001 Efficacy = 95.0 % -
CHEMBL390020 Efficacy = 100.0 % -
CHEMBL243999 Efficacy = 94.0 % -
CHEMBL243791 Efficacy = 96.0 % -
CHEMBL243970 Efficacy = 95.0 % -
CHEMBL243790 Efficacy = 95.0 % -
CHEMBL389907 Efficacy = 97.0 % -
CHEMBL395291 Efficacy = 95.0 % -
CHEMBL244000 Efficacy = 96.0 % -
CHEMBL243789 Efficacy = 88.0 % -