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Assay Detail

CHEMBL708494

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

Functional
Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-estradiol (in vitro)
ChEMBL ↗
73
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type MCF7
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866) ↗
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene.
Grese TA, Cho S, Finley DR, Godfrey AG, Jones CD, Lugar CW, Martin MJ, Matsumoto K, Pennington LD, Winter MA, Adrian MD, Cole HW, Magee DE, Phillips DL, Rowley ER, Short LL, Glasebrook AL, Bryant HU.
J Med Chem (1997) 40 : 146 -167
PubMed 9003514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 73 7.56 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81 RALOXIFENE 4.0 1 9.70
CHEMBL48021 — — 1 9.52
CHEMBL2137046 — — 1 9.30
CHEMBL44492 — — 1 9.15
CHEMBL43779 — — 1 9.10
CHEMBL44940 — — 1 9.10
CHEMBL544964 — — 1 9.00
CHEMBL43775 — — 1 9.00
CHEMBL64692 — — 1 8.70
CHEMBL44633 — — 1 8.70
CHEMBL48079 — — 1 8.70
CHEMBL44158 — — 1 8.70
CHEMBL540790 — — 1 8.64
CHEMBL47821 — — 1 8.64
CHEMBL295111 — — 1 8.60
CHEMBL47944 — — 1 8.60
CHEMBL556034 — — 1 8.60
CHEMBL47358 — — 1 8.52
CHEMBL296875 — — 1 8.52
CHEMBL295903 — — 1 8.49
CHEMBL416810 — — 1 8.30
CHEMBL44812 — — 1 8.30
CHEMBL47012 — — 1 8.30
CHEMBL297549 — — 1 8.15
CHEMBL46408 — — 1 8.00
CHEMBL46937 — — 1 8.00
CHEMBL46806 — — 1 8.00
CHEMBL47811 — — 1 7.70
CHEMBL46921 — — 1 7.70
CHEMBL46409 — — 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81 RALOXIFENE IC50 = 0.2 nM 9.70
CHEMBL48021 — IC50 = 0.3 nM 9.52
CHEMBL2137046 — IC50 = 0.5 nM 9.30
CHEMBL44492 — IC50 = 0.7 nM 9.15
CHEMBL43779 — IC50 = 0.8 nM 9.10
CHEMBL44940 — IC50 = 0.8 nM 9.10
CHEMBL544964 — IC50 = 1.0 nM 9.00
CHEMBL43775 — IC50 = 1.0 nM 9.00
CHEMBL64692 — IC50 = 2.0 nM 8.70
CHEMBL44633 — IC50 = 2.0 nM 8.70
CHEMBL48079 — IC50 = 2.0 nM 8.70
CHEMBL44158 — IC50 = 2.0 nM 8.70
CHEMBL540790 — IC50 = 2.3 nM 8.64
CHEMBL47821 — IC50 = 2.3 nM 8.64
CHEMBL556034 — IC50 = 2.5 nM 8.60
CHEMBL47944 — IC50 = 2.5 nM 8.60
CHEMBL295111 — IC50 = 2.5 nM 8.60
CHEMBL47358 — IC50 = 3.0 nM 8.52
CHEMBL296875 — IC50 = 3.0 nM 8.52
CHEMBL295903 — IC50 = 3.2 nM 8.49
CHEMBL416810 — IC50 = 5.0 nM 8.30
CHEMBL44812 — IC50 = 5.0 nM 8.30
CHEMBL47012 — IC50 = 5.0 nM 8.30
CHEMBL297549 — IC50 = 7.0 nM 8.15
CHEMBL46806 — IC50 = 10.0 nM 8.00
CHEMBL46937 — IC50 = 10.0 nM 8.00
CHEMBL46408 — IC50 = 10.0 nM 8.00
CHEMBL47811 — IC50 = 20.0 nM 7.70
CHEMBL46921 — IC50 = 20.0 nM 7.70
CHEMBL46409 — IC50 = 20.0 nM 7.70
CHEMBL47247 — IC50 = 20.0 nM 7.70
CHEMBL47553 — IC50 = 30.0 nM 7.52
CHEMBL544723 — IC50 = 30.0 nM 7.52
CHEMBL297782 — IC50 = 30.0 nM 7.52
CHEMBL416088 — IC50 = 32.0 nM 7.50
CHEMBL43936 — IC50 = 35.0 nM 7.46
CHEMBL538492 — IC50 = 35.0 nM 7.46
CHEMBL45461 — IC50 = 40.0 nM 7.40
CHEMBL47217 — IC50 = 50.0 nM 7.30
CHEMBL544251 — IC50 = 50.0 nM 7.30
CHEMBL297996 — IC50 = 50.0 nM 7.30
CHEMBL297813 — IC50 = 60.0 nM 7.22
CHEMBL296226 — IC50 = 80.0 nM 7.10
CHEMBL295907 — IC50 = 100.0 nM 7.00
CHEMBL44643 — IC50 = 100.0 nM 7.00
CHEMBL44797 — IC50 = 100.0 nM 7.00
CHEMBL42018 — IC50 = 100.0 nM 7.00
CHEMBL45120 — IC50 = 100.0 nM 7.00
CHEMBL1160091 — IC50 = 100.0 nM 7.00
CHEMBL296759 — IC50 = 100.0 nM 7.00