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Assay Detail

CHEMBL940098

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

Functional
Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
Rewinkel J, Enthoven M, Golstein I, van der Rijst M, Scholten A, van Tilborg M, de Weys D, Wisse J, Hamersma H.
Bioorg Med Chem (2008) 16 : 2753 -2763
PubMed 18243712 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 9.00 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410304 1 9.89
CHEMBL260538 ULIPRISTAL ACETATE 4.0 1 9.70
CHEMBL267431 ASOPRISNIL 3.0 1 9.70
CHEMBL410923 1 9.57
CHEMBL259879 1 9.48
CHEMBL411522 1 9.37
CHEMBL258522 1 9.33
CHEMBL260330 1 9.26
CHEMBL260764 1 9.22
CHEMBL409661 1 9.21
CHEMBL260869 1 9.20
CHEMBL408424 1 9.12
CHEMBL407371 1 9.01
CHEMBL411086 1 8.89
CHEMBL409905 1 8.60
CHEMBL268788 1 8.50
CHEMBL411063 1 8.49
CHEMBL438593 1 8.44
CHEMBL406439 1 8.10
CHEMBL258521 1 8.07
CHEMBL261650 1 7.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410304 IC50 = 0.13 nM 9.89
CHEMBL260538 ULIPRISTAL ACETATE IC50 = 0.2 nM 9.70
CHEMBL267431 ASOPRISNIL IC50 = 0.2 nM 9.70
CHEMBL410923 IC50 = 0.27 nM 9.57
CHEMBL259879 IC50 = 0.33 nM 9.48
CHEMBL411522 IC50 = 0.43 nM 9.37
CHEMBL258522 IC50 = 0.47 nM 9.33
CHEMBL260330 IC50 = 0.55 nM 9.26
CHEMBL260764 IC50 = 0.6 nM 9.22
CHEMBL409661 IC50 = 0.61 nM 9.21
CHEMBL260869 IC50 = 0.63 nM 9.20
CHEMBL408424 IC50 = 0.75 nM 9.12
CHEMBL407371 IC50 = 0.98 nM 9.01
CHEMBL411086 IC50 = 1.3 nM 8.89
CHEMBL409905 IC50 = 2.5 nM 8.60
CHEMBL268788 IC50 = 3.14 nM 8.50
CHEMBL411063 IC50 = 3.25 nM 8.49
CHEMBL438593 IC50 = 3.64 nM 8.44
CHEMBL406439 IC50 = 7.89 nM 8.10
CHEMBL258521 IC50 = 8.48 nM 8.07
CHEMBL261650 IC50 = 14.8 nM 7.83