Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1786326

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

Binding
Inhibition of human recombinant iNOS by microtiter plate assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Nitric oxide synthase, inducible (CHEMBL4481)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.
Young RJ, Alderton W, Angell AD, Beswick PJ, Brown D, Chambers CL, Crowe MC, Dawson J, Hamlett CC, Hodgson ST, Kleanthous S, Knowles RG, Russell LJ, Stocker R, Woolven JM.
Bioorg Med Chem Lett (2011) 21 : 3037 -3040
PubMed 21482467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.77 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1783094 1 7.52
CHEMBL1783097 1 6.92
CHEMBL1783093 1 6.75
CHEMBL1783095 1 6.70
CHEMBL1783072 CYCLOBUTANECARBOXIMIDAMIDE 1 6.42
CHEMBL1783092 1 6.16
CHEMBL1783071 CYCLOPROPANECARBOXIMIDAMIDE 1 6.10
CHEMBL114551 GW-274150 2.0 1 5.85
CHEMBL1229853 CYCLOPENTANECARBOXIMIDAMIDE 1 5.36
CHEMBL1783091 1 5.28
CHEMBL1783090 1 5.05
CHEMBL1783098 1 5.03
CHEMBL1783096 1 4.85
CHEMBL1783074 1 4.29
CHEMBL1783089 1 4.24
CHEMBL1783073 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1783094 IC50 = 30.0 nM 7.52
CHEMBL1783097 IC50 = 120.0 nM 6.92
CHEMBL1783093 IC50 = 180.0 nM 6.75
CHEMBL1783095 IC50 = 200.0 nM 6.70
CHEMBL1783072 CYCLOBUTANECARBOXIMIDAMIDE IC50 = 380.0 nM 6.42
CHEMBL1783092 IC50 = 700.0 nM 6.16
CHEMBL1783071 CYCLOPROPANECARBOXIMIDAMIDE IC50 = 790.0 nM 6.10
CHEMBL114551 GW-274150 IC50 = 1400.0 nM 5.85
CHEMBL1229853 CYCLOPENTANECARBOXIMIDAMIDE IC50 = 4400.0 nM 5.36
CHEMBL1783091 IC50 = 5300.0 nM 5.28
CHEMBL1783090 IC50 = 8900.0 nM 5.05
CHEMBL1783098 IC50 = 9400.0 nM 5.03
CHEMBL1783096 IC50 = 14000.0 nM 4.85
CHEMBL1783074 IC50 = 51000.0 nM 4.29
CHEMBL1783089 IC50 = 58000.0 nM 4.24
CHEMBL1783073 IC50 > 100000.0 nM -