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Assay Detail

CHEMBL3750679

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

Binding
Inhibition of recombinant rat CYP11B2 using 11-deoxycorticosterone as substrate after 2 hrs by scintillation proximity assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 11B2, mitochondrial (CHEMBL3237)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
Papillon JP, Lou C, Singh AK, Adams CM, Ksander GM, Beil ME, Chen W, Leung-Chu J, Fu F, Gan L, Hu CW, Jeng AY, LaSala D, Liang G, Rigel DF, Russell KS, Vest JA, Watson C.
J Med Chem (2015) 58 : 9382 -9394
PubMed 26540564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.00 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3746175 1 5.70
CHEMBL3746125 1 5.41
CHEMBL3747269 1 5.10
CHEMBL3746868 1 4.96
CHEMBL3747562 1 4.56
CHEMBL3747069 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3746175 IC50 = 2000.0 nM 5.70
CHEMBL3746125 IC50 = 3900.0 nM 5.41
CHEMBL3747269 IC50 = 8000.0 nM 5.10
CHEMBL3746868 IC50 = 10900.0 nM 4.96
CHEMBL3747562 IC50 = 27400.0 nM 4.56
CHEMBL3747069 IC50 = 53100.0 nM 4.28