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Assay Detail

CHEMBL4031199

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

Binding
Displacement of fluormone labelled PL Red from human recombinant progesterone receptor after 1 to 6 hrs ligand by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Hemmerling M, Nilsson S, Edman K, Eirefelt S, Russell W, Hendrickx R, Johnsson E, Kärrman Mårdh C, Berger M, Rehwinkel H, Abrahamsson A, Dahmén J, Eriksson AR, Gabos B, Henriksson K, Hossain N, Ivanova S, Jansson AH, Jensen TJ, Jerre A, Johansson H, Klingstedt T, Lepistö M, Lindsjö M, Mile I, Nikitidis G, Steele J, Tehler U, Wissler L, Hansson T.
J Med Chem (2017) 60 : 8591 -8605
PubMed 28937774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.75 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1473 FLUTICASONE PROPIONATE 4.0 1 7.68
CHEMBL1676 FLUTICASONE FUROATE 4.0 1 7.68
CHEMBL1370 BUDESONIDE 4.0 1 7.55
CHEMBL4072756 AZD-5423 2.0 1 5.75
CHEMBL3666813 1 5.08
CHEMBL3666805 1 -
CHEMBL3666814 1 -
CHEMBL3666807 VELSECORAT 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1473 FLUTICASONE PROPIONATE IC50 = 21.0 nM 7.68
CHEMBL1676 FLUTICASONE FUROATE IC50 = 21.0 nM 7.68
CHEMBL1370 BUDESONIDE IC50 = 28.0 nM 7.55
CHEMBL4072756 AZD-5423 IC50 = 1760.0 nM 5.75
CHEMBL3666813 IC50 = 8280.0 nM 5.08
CHEMBL3666805 IC50 > 10000.0 nM -
CHEMBL3666814 IC50 > 10000.0 nM -
CHEMBL3666807 VELSECORAT IC50 > 10000.0 nM -