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Assay Detail

CHEMBL3293049

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

Binding
Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycorticosterone as substrate
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type V79MZh
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 11B2, mitochondrial (CHEMBL2722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.
Yin L, Hu Q, Emmerich J, Lo MM, Metzger E, Ali A, Hartmann RW.
J Med Chem (2014) 57 : 5179 -5189
PubMed 24899257 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.57 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099695 OSILODROSTAT 4.0 1 9.70
CHEMBL3287192 1 9.22
CHEMBL3287178 1 9.15
CHEMBL9298 FADROZOLE 2.0 1 9.10
CHEMBL1765205 1 8.96
CHEMBL3287193 1 8.77
CHEMBL3287188 1 8.66
CHEMBL3287179 1 8.55
CHEMBL3287187 1 8.52
CHEMBL3287194 1 7.89
CHEMBL3287189 1 7.85
CHEMBL3287185 1 7.80
CHEMBL3287190 1 7.64
CHEMBL3287180 1 7.52
CHEMBL3287184 1 7.44
CHEMBL3287186 1 7.26
CHEMBL3287169 1 7.22
CHEMBL3287183 1 7.21
CHEMBL3287191 1 7.11
CHEMBL3287181 1 6.82
CHEMBL3287170 1 6.64
CHEMBL3287182 1 6.37
CHEMBL3286405 1 6.22
CHEMBL3287171 1 5.89
CHEMBL3287175 1 5.84
CHEMBL3287174 1 5.55
CHEMBL3287176 1 5.51
CHEMBL3287177 1 -
CHEMBL3287173 1 -
CHEMBL3287172 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099695 OSILODROSTAT IC50 = 0.2 nM 9.70
CHEMBL3287192 IC50 = 0.6 nM 9.22
CHEMBL3287178 IC50 = 0.7 nM 9.15
CHEMBL9298 FADROZOLE IC50 = 0.8 nM 9.10
CHEMBL1765205 IC50 = 1.1 nM 8.96
CHEMBL3287193 IC50 = 1.7 nM 8.77
CHEMBL3287188 IC50 = 2.2 nM 8.66
CHEMBL3287179 IC50 = 2.8 nM 8.55
CHEMBL3287187 IC50 = 3.0 nM 8.52
CHEMBL3287194 IC50 = 13.0 nM 7.89
CHEMBL3287189 IC50 = 14.0 nM 7.85
CHEMBL3287185 IC50 = 16.0 nM 7.80
CHEMBL3287190 IC50 = 23.0 nM 7.64
CHEMBL3287180 IC50 = 30.0 nM 7.52
CHEMBL3287184 IC50 = 36.0 nM 7.44
CHEMBL3287186 IC50 = 55.0 nM 7.26
CHEMBL3287169 IC50 = 60.0 nM 7.22
CHEMBL3287183 IC50 = 61.0 nM 7.21
CHEMBL3287191 IC50 = 77.0 nM 7.11
CHEMBL3287181 IC50 = 152.0 nM 6.82
CHEMBL3287170 IC50 = 228.0 nM 6.64
CHEMBL3287182 IC50 = 426.0 nM 6.37
CHEMBL3286405 IC50 = 607.0 nM 6.22
CHEMBL3287171 IC50 = 1285.0 nM 5.89
CHEMBL3287175 IC50 = 1433.0 nM 5.84
CHEMBL3287174 IC50 = 2833.0 nM 5.55
CHEMBL3287176 IC50 = 3070.0 nM 5.51
CHEMBL3287177 IC50 > 5000.0 nM -
CHEMBL3287173 IC50 > 5000.0 nM -
CHEMBL3287172 IC50 > 5000.0 nM -