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Assay Detail

CHEMBL678091

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Binding
Inhibitory activity against human endothelial nitric oxide synthase (eNOS) isoenzyme.
ChEMBL ↗
50
Total Activities
50
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

N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.
Collins JL, Shearer BG, Oplinger JA, Lee S, Garvey EP, Salter M, Duffy C, Burnette TC, Furfine ES.
J Med Chem (1998) 41 : 2858 -2871
PubMed 9667974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 5.08 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL227744 NITROARGININE 1.0 1 7.52
CHEMBL555794 — — 1 6.50
CHEMBL552825 — — 1 6.46
CHEMBL555715 — — 1 6.40
CHEMBL256147 TILARGININE 3.0 1 6.40
CHEMBL555584 — — 1 5.96
CHEMBL539793 — — 1 5.72
CHEMBL540048 — — 1 5.52
CHEMBL542433 — — 1 5.42
CHEMBL542432 — — 1 5.21
CHEMBL542674 — — 1 5.10
CHEMBL543142 — — 1 5.10
CHEMBL554201 — — 1 5.04
CHEMBL545025 — — 1 5.02
CHEMBL553453 — — 1 4.96
CHEMBL544793 — — 1 4.89
CHEMBL542675 — — 1 4.89
CHEMBL542676 — — 1 4.89
CHEMBL542912 — — 1 4.85
CHEMBL542431 — — 1 4.82
CHEMBL544317 — — 1 4.77
CHEMBL542677 — — 1 4.77
CHEMBL554192 — — 1 4.58
CHEMBL542429 — — 1 4.57
CHEMBL543381 — — 1 4.57
CHEMBL538767 — — 1 4.48
CHEMBL543380 — — 1 4.44
CHEMBL544090 — — 1 4.42
CHEMBL544093 — — 1 4.42
CHEMBL544557 — — 1 4.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL227744 NITROARGININE Ki = 30.0 nM 7.52
CHEMBL555794 — Ki = 320.0 nM 6.50
CHEMBL552825 — Ki = 350.0 nM 6.46
CHEMBL555715 — Ki = 400.0 nM 6.40
CHEMBL256147 TILARGININE Ki = 400.0 nM 6.40
CHEMBL555584 — Ki = 1100.0 nM 5.96
CHEMBL539793 — Ki = 1900.0 nM 5.72
CHEMBL540048 — Ki = 3000.0 nM 5.52
CHEMBL542433 — Ki = 3800.0 nM 5.42
CHEMBL542432 — Ki = 6200.0 nM 5.21
CHEMBL542674 — Ki = 8000.0 nM 5.10
CHEMBL543142 — Ki = 7900.0 nM 5.10
CHEMBL554201 — Ki = 9100.0 nM 5.04
CHEMBL545025 — Ki = 9500.0 nM 5.02
CHEMBL553453 — Ki = 11000.0 nM 4.96
CHEMBL544793 — Ki = 13000.0 nM 4.89
CHEMBL542676 — Ki = 13000.0 nM 4.89
CHEMBL542675 — Ki = 13000.0 nM 4.89
CHEMBL542912 — Ki = 14000.0 nM 4.85
CHEMBL542431 — Ki = 15000.0 nM 4.82
CHEMBL544317 — Ki = 17000.0 nM 4.77
CHEMBL542677 — Ki = 17000.0 nM 4.77
CHEMBL554192 — Ki = 26000.0 nM 4.58
CHEMBL542429 — Ki = 27000.0 nM 4.57
CHEMBL543381 — Ki = 27000.0 nM 4.57
CHEMBL538767 — Ki = 33000.0 nM 4.48
CHEMBL543380 — Ki = 36000.0 nM 4.44
CHEMBL544090 — Ki = 38000.0 nM 4.42
CHEMBL544093 — Ki = 38000.0 nM 4.42
CHEMBL544557 — Ki = 39000.0 nM 4.41
CHEMBL545023 — Ki = 43000.0 nM 4.37
CHEMBL543143 — Ki = 44000.0 nM 4.36
CHEMBL554248 — Ki = 46000.0 nM 4.34
CHEMBL553132 — Ki = 46000.0 nM 4.34
CHEMBL544788 — Ki = 75000.0 nM 4.12
CHEMBL557337 — Ki > 50000.0 nM -
CHEMBL542910 — Ki > 50000.0 nM -
CHEMBL540299 — Ki > 50000.0 nM -
CHEMBL540558 — Ki > 50000.0 nM -
CHEMBL544789 — Ki > 50000.0 nM -
CHEMBL538021 — Ki > 50000.0 nM -
CHEMBL555389 — Ki > 50000.0 nM -
CHEMBL542913 — Ki > 50000.0 nM -
CHEMBL542678 — Ki > 50000.0 nM -
CHEMBL544790 — Ki > 50000.0 nM -
CHEMBL544559 — Ki > 50000.0 nM -
CHEMBL539802 — Ki > 50000.0 nM -
CHEMBL545256 — Ki > 50000.0 nM -
CHEMBL542909 — Ki > 50000.0 nM -
CHEMBL540555 — Ki > 50000.0 nM -