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Assay Detail

CHEMBL947334

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Functional
Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs
ChEMBL ↗
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T47D
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Progesterone receptor (CHEMBL208) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Syntheses and antigestagenic activity of mifepristone derivatives.
Hödl C, Raunegger K, Strommer R, Ecker GF, Kunert O, Sturm S, Seger C, Haslinger E, Steiner R, Strauss WS, Schramm HW.
J Med Chem (2009) 52 : 1268 -1274
PubMed 19216549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 9.10 10.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 10.35
CHEMBL455411 — — 1 10.22
CHEMBL221686 — — 1 10.02
CHEMBL489300 — — 1 9.92
CHEMBL453381 — — 1 9.82
CHEMBL507916 — — 1 9.80
CHEMBL455175 — — 1 9.80
CHEMBL1608 DESMETHYLMIFEPRISTONE — 1 9.77
CHEMBL455530 — — 1 9.77
CHEMBL507253 — — 1 9.77
CHEMBL451680 — — 1 9.60
CHEMBL449900 — — 1 9.57
CHEMBL510869 — — 1 9.57
CHEMBL490088 — — 1 9.57
CHEMBL504799 — — 1 9.40
CHEMBL509832 — — 1 9.36
CHEMBL452860 — — 1 9.36
CHEMBL444027 — — 1 9.34
CHEMBL504252 — — 1 9.34
CHEMBL499452 — — 1 9.33
CHEMBL445043 — — 1 9.26
CHEMBL450052 — — 1 9.20
CHEMBL493845 — — 1 9.18
CHEMBL455176 — — 1 9.16
CHEMBL454167 — — 1 9.14
CHEMBL453361 — — 1 9.10
CHEMBL505959 — — 1 9.05
CHEMBL454435 — — 1 9.00
CHEMBL506443 — — 1 8.92
CHEMBL490087 — — 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.045 nM 10.35
CHEMBL455411 — IC50 = 0.06 nM 10.22
CHEMBL221686 — IC50 = 0.095 nM 10.02
CHEMBL489300 — IC50 = 0.12 nM 9.92
CHEMBL453381 — IC50 = 0.15 nM 9.82
CHEMBL507916 — IC50 = 0.16 nM 9.80
CHEMBL455175 — IC50 = 0.16 nM 9.80
CHEMBL1608 DESMETHYLMIFEPRISTONE IC50 = 0.17 nM 9.77
CHEMBL455530 — IC50 = 0.17 nM 9.77
CHEMBL507253 — IC50 = 0.17 nM 9.77
CHEMBL451680 — IC50 = 0.25 nM 9.60
CHEMBL449900 — IC50 = 0.27 nM 9.57
CHEMBL490088 — IC50 = 0.27 nM 9.57
CHEMBL510869 — IC50 = 0.27 nM 9.57
CHEMBL504799 — IC50 = 0.4 nM 9.40
CHEMBL509832 — IC50 = 0.44 nM 9.36
CHEMBL452860 — IC50 = 0.44 nM 9.36
CHEMBL444027 — IC50 = 0.46 nM 9.34
CHEMBL504252 — IC50 = 0.46 nM 9.34
CHEMBL499452 — IC50 = 0.47 nM 9.33
CHEMBL445043 — IC50 = 0.55 nM 9.26
CHEMBL450052 — IC50 = 0.63 nM 9.20
CHEMBL493845 — IC50 = 0.66 nM 9.18
CHEMBL455176 — IC50 = 0.69 nM 9.16
CHEMBL454167 — IC50 = 0.73 nM 9.14
CHEMBL453361 — IC50 = 0.79 nM 9.10
CHEMBL505959 — IC50 = 0.9 nM 9.05
CHEMBL454435 — IC50 = 1.0 nM 9.00
CHEMBL506443 — IC50 = 1.2 nM 8.92
CHEMBL490087 — IC50 = 1.3 nM 8.89
CHEMBL459203 — IC50 = 1.4 nM 8.85
CHEMBL449367 — IC50 = 1.55 nM 8.81
CHEMBL454121 — IC50 = 1.7 nM 8.77
CHEMBL454224 — IC50 = 1.8 nM 8.74
CHEMBL446933 — IC50 = 2.1 nM 8.68
CHEMBL451127 — IC50 = 2.2 nM 8.66
CHEMBL453382 — IC50 = 34.0 nM 7.47
CHEMBL503056 — IC50 = 72.0 nM 7.14
CHEMBL461357 — IC50 = 72.0 nM 7.14
CHEMBL505267 — IC50 = 78.0 nM 7.11
CHEMBL500992 — IC50 = 100.0 nM 7.00