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Assay Detail

CHEMBL768145

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

Binding
Binding affinity against Progesterone receptor in human TE85 osteosarcoma cells was determined using (Z)-[125I]-17-alpha-(2-iodovinyl)-19-nor-testosterone as radioligand
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal progesterone receptor ligands. 2. High-affinity ligands with selectivity for bone cell progesterone receptors.
Combs DW, Reese K, Cornelius LA, Gunnet JW, Cryan EV, Granger KS, Jordan JJ, Demarest KT.
J Med Chem (1995) 38 : 4880 -4884
PubMed 8523400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.09 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1162 NORETHINDRONE 4.0 1 8.49
CHEMBL103 PROGESTERONE 4.0 1 7.77
CHEMBL145224 1 7.76
CHEMBL144680 1 7.62
CHEMBL262171 1 7.42
CHEMBL144694 1 7.32
CHEMBL145544 1 7.21
CHEMBL357848 1 7.15
CHEMBL356741 1 7.12
CHEMBL144068 1 7.08
CHEMBL148070 1 7.01
CHEMBL144321 1 6.77
CHEMBL144815 1 6.57
CHEMBL144345 1 6.38
CHEMBL144803 1 6.29
CHEMBL145346 1 6.28
CHEMBL359228 1 6.24
CHEMBL144039 1 -
CHEMBL144180 1 -
CHEMBL145254 1 -
CHEMBL343409 1 -
CHEMBL342508 1 -
CHEMBL144038 1 -
CHEMBL358274 1 -
CHEMBL144289 1 -
CHEMBL359431 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1162 NORETHINDRONE IC50 = 3.2 nM 8.49
CHEMBL103 PROGESTERONE IC50 = 17.0 nM 7.77
CHEMBL145224 IC50 = 17.5 nM 7.76
CHEMBL144680 IC50 = 24.0 nM 7.62
CHEMBL262171 IC50 = 38.2 nM 7.42
CHEMBL144694 IC50 = 48.2 nM 7.32
CHEMBL145544 IC50 = 62.4 nM 7.21
CHEMBL357848 IC50 = 70.6 nM 7.15
CHEMBL356741 IC50 = 75.3 nM 7.12
CHEMBL144068 IC50 = 84.0 nM 7.08
CHEMBL148070 IC50 = 98.0 nM 7.01
CHEMBL144321 IC50 = 170.0 nM 6.77
CHEMBL144815 IC50 = 270.0 nM 6.57
CHEMBL144345 IC50 = 416.0 nM 6.38
CHEMBL144803 IC50 = 515.0 nM 6.29
CHEMBL145346 IC50 = 521.0 nM 6.28
CHEMBL359228 IC50 = 570.0 nM 6.24
CHEMBL144039 IC50 > 1000.0 nM -
CHEMBL144180 IC50 > 1000.0 nM -
CHEMBL145254 IC50 > 1000.0 nM -
CHEMBL343409 IC50 > 1000.0 nM -
CHEMBL342508 IC50 > 1000.0 nM -
CHEMBL144038 IC50 > 1000.0 nM -
CHEMBL358274 IC50 > 1000.0 nM -
CHEMBL144289 IC50 > 1000.0 nM -
CHEMBL359431 IC50 > 1000.0 nM -