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Assay Detail

CHEMBL765846

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

Binding
The binding affinity measured using baculovirus-expressed hPR-A in sf21 cells.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.
Edwards JP, West SJ, Marschke KB, Mais DE, Gottardis MM, Jones TK.
J Med Chem (1998) 41 : 303 -310
PubMed 9464361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 9.07 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416411 1 9.49
CHEMBL106994 1 9.49
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 9.47
CHEMBL322485 1 9.47
CHEMBL320164 1 9.43
CHEMBL104183 1 9.32
CHEMBL94749 1 9.31
CHEMBL94753 1 9.30
CHEMBL319915 1 9.26
CHEMBL322575 1 9.23
CHEMBL322576 1 9.23
CHEMBL286595 1 9.15
CHEMBL318409 1 9.13
CHEMBL418990 1 9.11
CHEMBL322312 1 9.03
CHEMBL431807 1 8.96
CHEMBL320632 1 8.89
CHEMBL104347 1 8.89
CHEMBL1162 NORETHINDRONE 4.0 1 8.73
CHEMBL104037 1 8.66
CHEMBL107998 1 8.62
CHEMBL104451 1 8.57
CHEMBL108230 1 8.57
CHEMBL103 PROGESTERONE 4.0 1 8.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416411 Ki = 0.32 nM 9.49
CHEMBL106994 Ki = 0.32 nM 9.49
CHEMBL717 MEDROXYPROGESTERONE ACETATE Ki = 0.34 nM 9.47
CHEMBL322485 Ki = 0.34 nM 9.47
CHEMBL320164 Ki = 0.37 nM 9.43
CHEMBL104183 Ki = 0.48 nM 9.32
CHEMBL94749 Ki = 0.49 nM 9.31
CHEMBL94753 Ki = 0.5 nM 9.30
CHEMBL319915 Ki = 0.55 nM 9.26
CHEMBL322575 Ki = 0.59 nM 9.23
CHEMBL322576 Ki = 0.59 nM 9.23
CHEMBL286595 Ki = 0.7 nM 9.15
CHEMBL318409 Ki = 0.74 nM 9.13
CHEMBL418990 Ki = 0.78 nM 9.11
CHEMBL322312 Ki = 0.93 nM 9.03
CHEMBL431807 Ki = 1.1 nM 8.96
CHEMBL320632 Ki = 1.3 nM 8.89
CHEMBL104347 Ki = 1.3 nM 8.89
CHEMBL1162 NORETHINDRONE Ki = 1.87 nM 8.73
CHEMBL104037 Ki = 2.2 nM 8.66
CHEMBL107998 Ki = 2.4 nM 8.62
CHEMBL104451 Ki = 2.7 nM 8.57
CHEMBL108230 Ki = 2.7 nM 8.57
CHEMBL103 PROGESTERONE Ki = 3.5 nM 8.46