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Assay Detail

CHEMBL940096

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

Functional
Agonist activity at human PRB expressed in CHO cells
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
EC50 21 9.20 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260869 1 9.92
CHEMBL260330 1 9.82
CHEMBL410923 1 9.70
CHEMBL260764 1 9.64
CHEMBL259879 1 9.54
CHEMBL438593 1 9.44
CHEMBL410304 1 9.31
CHEMBL258521 1 9.31
CHEMBL411522 1 9.29
CHEMBL409661 1 9.18
CHEMBL407371 1 9.13
CHEMBL408424 1 9.09
CHEMBL268788 1 9.00
CHEMBL258522 1 8.96
CHEMBL411086 1 8.95
CHEMBL406439 1 8.89
CHEMBL411063 1 8.60
CHEMBL261650 1 8.59
CHEMBL409905 1 8.40
CHEMBL267431 ASOPRISNIL 3.0 1 -
CHEMBL260538 ULIPRISTAL ACETATE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260869 EC50 = 0.12 nM 9.92
CHEMBL260330 EC50 = 0.15 nM 9.82
CHEMBL410923 EC50 = 0.2 nM 9.70
CHEMBL260764 EC50 = 0.23 nM 9.64
CHEMBL259879 EC50 = 0.29 nM 9.54
CHEMBL438593 EC50 = 0.36 nM 9.44
CHEMBL410304 EC50 = 0.49 nM 9.31
CHEMBL258521 EC50 = 0.49 nM 9.31
CHEMBL411522 EC50 = 0.51 nM 9.29
CHEMBL409661 EC50 = 0.66 nM 9.18
CHEMBL407371 EC50 = 0.74 nM 9.13
CHEMBL408424 EC50 = 0.82 nM 9.09
CHEMBL268788 EC50 = 1.0 nM 9.00
CHEMBL258522 EC50 = 1.1 nM 8.96
CHEMBL411086 EC50 = 1.13 nM 8.95
CHEMBL406439 EC50 = 1.3 nM 8.89
CHEMBL411063 EC50 = 2.54 nM 8.60
CHEMBL261650 EC50 = 2.6 nM 8.59
CHEMBL409905 EC50 = 4.0 nM 8.40
CHEMBL267431 ASOPRISNIL EC50 > 100.0 nM -
CHEMBL260538 ULIPRISTAL ACETATE EC50 > 100.0 nM -