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Assay Detail

CHEMBL1763070

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Binding
Inhibition of NET
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).
Cheshire DR, Åberg A, Andersson GM, Andrews G, Beaton HG, Birkinshaw TN, Boughton-Smith N, Connolly S, Cook TR, Cooper A, Cooper SL, Cox D, Dixon J, Gensmantel N, Hamley PJ, Harrison R, Hartopp P, Käck H, Leeson PD, Luker T, Mete A, Millichip I, Nicholls DJ, Pimm AD, St-Gallay SA, Wallace AV.
Bioorg Med Chem Lett (2011) 21 : 2468 -2471
PubMed 21398123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.06 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762472 1 6.30
CHEMBL1762478 1 5.15
CHEMBL1762480 1 5.13
CHEMBL1762476 1 4.92
CHEMBL1762473 1 4.82
CHEMBL1762479 1 4.80
CHEMBL1762474 1 4.77
CHEMBL1762475 1 4.55
CHEMBL447183 1 -
CHEMBL1762470 1 -
CHEMBL1762471 1 -
CHEMBL1762477 1 -
CHEMBL1762481 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762472 IC50 = 500.0 nM 6.30
CHEMBL1762478 IC50 = 7100.0 nM 5.15
CHEMBL1762480 IC50 = 7400.0 nM 5.13
CHEMBL1762476 IC50 = 12000.0 nM 4.92
CHEMBL1762473 IC50 = 15000.0 nM 4.82
CHEMBL1762479 IC50 = 16000.0 nM 4.80
CHEMBL1762474 IC50 = 17000.0 nM 4.77
CHEMBL1762475 IC50 = 28000.0 nM 4.55
CHEMBL447183 IC50 - -
CHEMBL1762470 IC50 - -
CHEMBL1762471 IC50 = - nM -
CHEMBL1762477 IC50 - -
CHEMBL1762481 IC50 > 100000.0 nM -