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Assay Detail

CHEMBL766186

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

Binding
Displacement of [3H]progesterone from human Progesterone receptor A
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Kym PR, Kort ME, Coghlan MJ, Moore JL, Tang R, Ratajczyk JD, Larson DP, Elmore SW, Pratt JK, Stashko MA, Falls HD, Lin CW, Nakane M, Miller L, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Nguyen P, Lane BC.
J Med Chem (2003) 46 : 1016 -1030
PubMed 12620078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.50 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273658 1 8.12
CHEMBL7781 1 7.66
CHEMBL7987 1 7.54
CHEMBL8027 1 7.47
CHEMBL8639 1 7.45
CHEMBL8007 1 7.21
CHEMBL8637 1 7.00
CHEMBL8140 1 6.82
CHEMBL268239 1 6.72
CHEMBL7988 1 6.70
CHEMBL7843 1 6.70
CHEMBL266709 1 6.48
CHEMBL267231 1 6.46
CHEMBL267940 1 6.36
CHEMBL415309 1 6.35
CHEMBL274208 1 6.21
CHEMBL8209 1 5.84
CHEMBL266282 AL-43 1 5.75
CHEMBL266488 1 5.74
CHEMBL7671 1 5.62
CHEMBL440454 1 5.54
CHEMBL8055 1 5.51
CHEMBL8329 1 5.43
CHEMBL8394 1 5.32
CHEMBL7655 1 -
CHEMBL7817 1 -
CHEMBL131 PREDNISOLONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273658 Ki = 7.6 nM 8.12
CHEMBL7781 Ki = 22.0 nM 7.66
CHEMBL7987 Ki = 29.0 nM 7.54
CHEMBL8027 Ki = 34.0 nM 7.47
CHEMBL8639 Ki = 35.9 nM 7.45
CHEMBL8007 Ki = 61.0 nM 7.21
CHEMBL8637 Ki = 100.0 nM 7.00
CHEMBL8140 Ki = 150.0 nM 6.82
CHEMBL268239 Ki = 192.0 nM 6.72
CHEMBL7988 Ki = 200.0 nM 6.70
CHEMBL7843 Ki = 200.0 nM 6.70
CHEMBL266709 Ki = 330.0 nM 6.48
CHEMBL267231 Ki = 349.0 nM 6.46
CHEMBL267940 Ki = 435.0 nM 6.36
CHEMBL415309 Ki = 450.0 nM 6.35
CHEMBL274208 Ki = 610.0 nM 6.21
CHEMBL8209 Ki = 1460.0 nM 5.84
CHEMBL266282 AL-43 Ki = 1790.0 nM 5.75
CHEMBL266488 Ki = 1810.0 nM 5.74
CHEMBL7671 Ki = 2400.0 nM 5.62
CHEMBL440454 Ki = 2920.0 nM 5.54
CHEMBL8055 Ki = 3080.0 nM 5.51
CHEMBL8329 Ki = 3740.0 nM 5.43
CHEMBL8394 Ki = 4740.0 nM 5.32
CHEMBL7655 Ki > 5000.0 nM -
CHEMBL7817 Ki > 5000.0 nM -
CHEMBL131 PREDNISOLONE Ki > 5000.0 nM -