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Assay Detail

CHEMBL4153940

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

Binding
Inhibition of recombinant mouse iNOS using [3H]L-arginine as substrate preincubated for 15 mins followed by NADPH addition measured after 20 mins in presence of FMN/FAD by liquid scintillation counting method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nitric oxide synthase, inducible (CHEMBL3464)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of N-{3-[(ethanimidoylamino)methyl]benzyl}-l-prolinamide dihydrochloride: A new potent and selective inhibitor of the inducible nitric oxide synthase as a promising agent for the therapy of malignant glioma.
Maccallini C, Di Matteo M, Gallorini M, Montagnani M, Graziani V, Ammazzalorso A, Amoia P, De Filippis B, Di Silvestre S, Fantacuzzi M, Giampietro L, Potenza MA, Re N, Pandolfi A, Cataldi A, Amoroso R.
Eur J Med Chem (2018) 152 : 53 -64
PubMed 29689474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.50 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161447 1 7.24
CHEMBL107251 1400W 1 7.00
CHEMBL4171271 1 6.77
CHEMBL4169004 1 6.60
CHEMBL4160671 1 6.56
CHEMBL4169649 1 6.35
CHEMBL4177347 1 6.35
CHEMBL4173076 1 6.27
CHEMBL4176848 1 5.99
CHEMBL4166234 1 5.91
CHEMBL4171523 1 -
CHEMBL4163633 1 -
CHEMBL4161080 1 -
CHEMBL4172371 1 -
CHEMBL4164493 1 -
CHEMBL4170892 1 -
CHEMBL4162963 1 -
CHEMBL4160751 1 -
CHEMBL4171037 1 -
CHEMBL4161718 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161447 IC50 = 58.0 nM 7.24
CHEMBL107251 1400W IC50 = 101.0 nM 7.00
CHEMBL4171271 IC50 = 170.0 nM 6.77
CHEMBL4169004 IC50 = 253.0 nM 6.60
CHEMBL4160671 IC50 = 276.0 nM 6.56
CHEMBL4169649 IC50 = 446.0 nM 6.35
CHEMBL4177347 IC50 = 450.0 nM 6.35
CHEMBL4173076 IC50 = 534.0 nM 6.27
CHEMBL4176848 IC50 = 1025.0 nM 5.99
CHEMBL4166234 IC50 = 1229.0 nM 5.91
CHEMBL4171523 IC50 > 10000.0 nM -
CHEMBL4163633 IC50 > 10000.0 nM -
CHEMBL4161080 IC50 > 10000.0 nM -
CHEMBL4172371 IC50 > 10000.0 nM -
CHEMBL4164493 IC50 > 10000.0 nM -
CHEMBL4170892 IC50 > 10000.0 nM -
CHEMBL4162963 IC50 > 10000.0 nM -
CHEMBL4160751 IC50 > 10000.0 nM -
CHEMBL4171037 IC50 > 10000.0 nM -
CHEMBL4161718 IC50 > 10000.0 nM -