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Assay Detail

CHEMBL3750823

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

Binding
Inhibition of CYP11B2 in cynomolgus monkey adrenal homogenates assessed as inhibition of aldosterone secretion
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca fascicularis
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 4 8.04 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3746080 1 8.22
CHEMBL3746868 1 8.05
CHEMBL3747562 1 8.00
CHEMBL3747069 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3746080 IC50 = 6.0 nM 8.22
CHEMBL3746868 IC50 = 9.0 nM 8.05
CHEMBL3747562 IC50 = 10.0 nM 8.00
CHEMBL3747069 IC50 = 13.0 nM 7.89