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Assay Detail

CHEMBL889118

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

Binding
Displacement of [3H]estradiol from human recombinant ERalpha
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
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
Ki 17 9.36 10.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243970 1 10.04
CHEMBL390021 1 9.74
CHEMBL244206 1 9.70
CHEMBL390020 1 9.68
CHEMBL244205 1 9.62
CHEMBL243999 1 9.62
CHEMBL244000 1 9.49
CHEMBL243571 1 9.40
CHEMBL243789 1 9.33
CHEMBL395291 1 9.32
CHEMBL244001 1 9.24
CHEMBL389907 1 9.20
CHEMBL243791 1 9.14
CHEMBL244207 1 8.99
CHEMBL390448 1 8.96
CHEMBL243790 1 8.91
CHEMBL428926 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243970 Ki = 0.091 nM 10.04
CHEMBL390021 Ki = 0.18 nM 9.74
CHEMBL244206 Ki = 0.2 nM 9.70
CHEMBL390020 Ki = 0.21 nM 9.68
CHEMBL244205 Ki = 0.24 nM 9.62
CHEMBL243999 Ki = 0.24 nM 9.62
CHEMBL244000 Ki = 0.32 nM 9.49
CHEMBL243571 Ki = 0.4 nM 9.40
CHEMBL243789 Ki = 0.47 nM 9.33
CHEMBL395291 Ki = 0.48 nM 9.32
CHEMBL244001 Ki = 0.57 nM 9.24
CHEMBL389907 Ki = 0.63 nM 9.20
CHEMBL243791 Ki = 0.73 nM 9.14
CHEMBL244207 Ki = 1.03 nM 8.99
CHEMBL390448 Ki = 1.09 nM 8.96
CHEMBL243790 Ki = 1.22 nM 8.91
CHEMBL428926 Ki = 1.89 nM 8.72