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Assay Detail

CHEMBL4032161

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

Binding
Inhibition of human neuronal NOS expressed in Escherichia coli using L-arginine as substrate assessed as reduction in NO production by measuring oxidation of oxyHb to metHb measured for 6 mins by hemoglobin- NO capture assay
14
Total Activities
14
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 1 (CHEMBL3568)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker.
Do HT, Wang HY, Li H, Chreifi G, Poulos TL, Silverman RB.
J Med Chem (2017) 60 : 9360 -9375
PubMed 29091437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.03 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818373 1 7.89
CHEMBL4094689 1 7.52
CHEMBL4074188 1 7.37
CHEMBL4103382 1 7.26
CHEMBL4079135 1 7.19
CHEMBL4071288 1 7.09
CHEMBL4062639 1 7.08
CHEMBL4084332 1 7.00
CHEMBL4061573 1 6.44
CHEMBL4086997 1 6.29
CHEMBL4065564 1 6.22
CHEMBL4084484 1 -
CHEMBL4102437 1 -
CHEMBL4092089 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818373 Ki = 13.0 nM 7.89
CHEMBL4094689 Ki = 30.0 nM 7.52
CHEMBL4074188 Ki = 43.0 nM 7.37
CHEMBL4103382 Ki = 55.0 nM 7.26
CHEMBL4079135 Ki = 65.0 nM 7.19
CHEMBL4071288 Ki = 82.0 nM 7.09
CHEMBL4062639 Ki = 83.0 nM 7.08
CHEMBL4084332 Ki = 100.0 nM 7.00
CHEMBL4061573 Ki = 362.0 nM 6.44
CHEMBL4086997 Ki = 516.0 nM 6.29
CHEMBL4065564 Ki = 598.0 nM 6.22
CHEMBL4084484 Ki - -
CHEMBL4102437 Ki - -
CHEMBL4092089 Ki - -