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Assay Detail

CHEMBL763450

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Functional
Antagonist activity against human progesterone receptor (hPR) in T47D human breast cancer cell line
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type T47D
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.
Zhi L, Tegley CM, Pio B, West SJ, Marschke KB, Mais DE, Jones TK.
Bioorg Med Chem Lett (2000) 10 : 415 -418
PubMed 10743938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.96 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908373 ONAPRISTONE 2.0 1 8.48
CHEMBL133656 1 7.16
CHEMBL339399 1 7.15
CHEMBL134786 1 7.11
CHEMBL132193 1 7.10
CHEMBL337885 1 6.99
CHEMBL133794 1 6.98
CHEMBL335992 1 6.97
CHEMBL132195 1 6.92
CHEMBL132192 1 6.92
CHEMBL131855 1 6.91
CHEMBL133661 1 6.82
CHEMBL334890 1 6.82
CHEMBL538158 1 6.72
CHEMBL132950 1 6.60
CHEMBL134258 1 6.56
CHEMBL337199 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908373 ONAPRISTONE IC50 = 3.3 nM 8.48
CHEMBL133656 IC50 = 70.0 nM 7.16
CHEMBL339399 IC50 = 71.0 nM 7.15
CHEMBL134786 IC50 = 78.0 nM 7.11
CHEMBL132193 IC50 = 80.0 nM 7.10
CHEMBL337885 IC50 = 102.0 nM 6.99
CHEMBL133794 IC50 = 105.0 nM 6.98
CHEMBL335992 IC50 = 106.0 nM 6.97
CHEMBL132195 IC50 = 120.0 nM 6.92
CHEMBL132192 IC50 = 120.0 nM 6.92
CHEMBL131855 IC50 = 123.0 nM 6.91
CHEMBL133661 IC50 = 151.0 nM 6.82
CHEMBL334890 IC50 = 150.0 nM 6.82
CHEMBL538158 IC50 = 190.0 nM 6.72
CHEMBL132950 IC50 = 250.0 nM 6.60
CHEMBL134258 IC50 = 278.0 nM 6.56
CHEMBL337199 IC50 = 700.0 nM 6.16