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Assay Detail

CHEMBL651955

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

Binding
Binding affinity was determined on Human androgen receptor (hAR) using progesterone as radioligand.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.
Zhi L, Tegley CM, Kallel EA, Marschke KB, Mais DE, Gottardis MM, Jones TK.
J Med Chem (1998) 41 : 291 -302
PubMed 9464360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.06 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 8.54
CHEMBL103 PROGESTERONE 4.0 1 8.07
CHEMBL318513 1 6.10
CHEMBL102754 1 5.84
CHEMBL320690 1 5.82
CHEMBL103092 1 5.80
CHEMBL101914 1 5.73
CHEMBL102720 1 5.73
CHEMBL430855 1 5.67
CHEMBL102403 1 5.63
CHEMBL102541 1 5.59
CHEMBL286595 1 5.57
CHEMBL101907 1 5.46
CHEMBL317921 1 5.23
CHEMBL103232 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE Ki = 2.9 nM 8.54
CHEMBL103 PROGESTERONE Ki = 8.5 nM 8.07
CHEMBL318513 Ki = 795.0 nM 6.10
CHEMBL102754 Ki = 1457.0 nM 5.84
CHEMBL320690 Ki = 1526.0 nM 5.82
CHEMBL103092 Ki = 1581.0 nM 5.80
CHEMBL101914 Ki = 1856.0 nM 5.73
CHEMBL102720 Ki = 1860.0 nM 5.73
CHEMBL430855 Ki = 2138.0 nM 5.67
CHEMBL102403 Ki = 2330.0 nM 5.63
CHEMBL102541 Ki = 2584.0 nM 5.59
CHEMBL286595 Ki = 2685.0 nM 5.57
CHEMBL101907 Ki = 3499.0 nM 5.46
CHEMBL317921 Ki = 5831.0 nM 5.23
CHEMBL103232 Ki > 10000.0 nM -