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Assay Detail

CHEMBL678078

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Binding
inhibition of human endothelial constitutive Endothelial nitric oxide synthase (heNOS)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Nitric oxide synthase 3 (CHEMBL4803)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms.
Webber RK, Metz S, Moore WM, Connor JR, Currie MG, Fok KF, Hagen TJ, Hansen DW, Jerome GM, Manning PT, Pitzele BS, Toth MV, Trivedi M, Zupec ME, Tjoeng FS.
J Med Chem (1998) 41 : 96 -101
PubMed 9438025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.33 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269076 1 6.52
CHEMBL265672 1 6.22
CHEMBL6808 1 5.96
CHEMBL267038 1 5.70
CHEMBL6760 1 5.66
CHEMBL267167 1 5.52
CHEMBL269058 1 5.33
CHEMBL6643 1 5.28
CHEMBL6813 1 4.89
CHEMBL6875 1 4.36
CHEMBL268312 1 4.33
CHEMBL269330 1 4.24
CHEMBL7133 1 -
CHEMBL6656 1 -
CHEMBL6657 1 -
CHEMBL268294 1 -
CHEMBL266980 1 -
CHEMBL269560 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269076 IC50 = 300.0 nM 6.52
CHEMBL265672 IC50 = 600.0 nM 6.22
CHEMBL6808 IC50 = 1100.0 nM 5.96
CHEMBL267038 IC50 = 2000.0 nM 5.70
CHEMBL6760 IC50 = 2200.0 nM 5.66
CHEMBL267167 IC50 = 3000.0 nM 5.52
CHEMBL269058 IC50 = 4700.0 nM 5.33
CHEMBL6643 IC50 = 5300.0 nM 5.28
CHEMBL6813 IC50 = 13000.0 nM 4.89
CHEMBL6875 IC50 = 44000.0 nM 4.36
CHEMBL268312 IC50 = 47000.0 nM 4.33
CHEMBL269330 IC50 = 58000.0 nM 4.24
CHEMBL7133 IC50 = 142000.0 nM -
CHEMBL6656 IC50 = 218000.0 nM -
CHEMBL6657 IC50 > 100000.0 nM -
CHEMBL268294 IC50 > 100000.0 nM -
CHEMBL266980 IC50 > 100000.0 nM -
CHEMBL269560 IC50 = 375000.0 nM -