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Assay Detail

CHEMBL1803809

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

Binding
Inhibition of human iNOS assessed as inhibition of [3H]L-arginine to [3H]L-citrulline conversion by scintillation counting
23
Total Activities
23
Compounds Tested
2
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

Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.
Grädler U, Fuchss T, Ulrich WR, Boer R, Strub A, Hesslinger C, Anézo C, Diederichs K, Zaliani A.
Bioorg Med Chem Lett (2011) 21 : 4228 -4232
PubMed 21684157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.40 7.43
Ki 1 8.73 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800346 1 8.73
CHEMBL447183 1 7.43
CHEMBL1800534 1 7.41
CHEMBL1800533 1 7.26
CHEMBL1800347 1 7.15
CHEMBL1738840 1 7.09
CHEMBL59925 1 6.96
CHEMBL1800348 1 6.94
CHEMBL1800528 1 6.84
CHEMBL1800523 1 6.81
CHEMBL1800526 1 6.73
CHEMBL1800527 1 6.42
CHEMBL1800531 1 6.29
CHEMBL1800532 1 6.14
CHEMBL1800530 1 6.11
CHEMBL114551 GW-274150 2.0 1 5.85
CHEMBL1800529 1 5.64
CHEMBL7889 L-NIL 1 5.33
CHEMBL51478 1 4.97
CHEMBL1800349 1 4.31
CHEMBL1800524 1 -
CHEMBL1800525 1 -
CHEMBL1185460 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800346 Ki = 1.862 nM 8.73
CHEMBL447183 IC50 = 37.15 nM 7.43
CHEMBL1800534 IC50 = 38.9 nM 7.41
CHEMBL1800533 IC50 = 54.95 nM 7.26
CHEMBL1800347 IC50 = 70.79 nM 7.15
CHEMBL1738840 IC50 = 81.28 nM 7.09
CHEMBL59925 IC50 = 109.65 nM 6.96
CHEMBL1800348 IC50 = 114.82 nM 6.94
CHEMBL1800528 IC50 = 144.54 nM 6.84
CHEMBL1800523 IC50 = 154.88 nM 6.81
CHEMBL1800526 IC50 = 186.21 nM 6.73
CHEMBL1800527 IC50 = 380.19 nM 6.42
CHEMBL1800531 IC50 = 512.86 nM 6.29
CHEMBL1800532 IC50 = 724.44 nM 6.14
CHEMBL1800530 IC50 = 776.25 nM 6.11
CHEMBL114551 GW-274150 IC50 = 1412.54 nM 5.85
CHEMBL1800529 IC50 = 2290.87 nM 5.64
CHEMBL7889 L-NIL IC50 = 4677.35 nM 5.33
CHEMBL51478 IC50 = 10715.19 nM 4.97
CHEMBL1800349 IC50 = 48977.88 nM 4.31
CHEMBL1800524 IC50 > 100000.0 nM -
CHEMBL1800525 IC50 > 100000.0 nM -
CHEMBL1185460 IC50 > 100000.0 nM -