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Assay Detail

CHEMBL857231

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Functional
In vitro functional NK1 activity as inhibition of guinea pig bronchoconstriction
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Lung
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Substance-P receptor (CHEMBL3942)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.
Ting PC, Lee JF, Shih NY, Piwinski JJ, Anthes JC, Chapman RW, Rizzo CA, Hey JA, Ng K, Nomeir AA.
Bioorg Med Chem Lett (2002) 12 : 2125 -2128
PubMed 12127519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 7.95 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302329 1 8.20
CHEMBL304106 1 8.00
CHEMBL66441 1 8.00
CHEMBL68060 1 8.00
CHEMBL441252 1 8.00
CHEMBL57993 1 8.00
CHEMBL66332 1 7.90
CHEMBL67171 1 7.90
CHEMBL60504 1 7.80
CHEMBL66635 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302329 Kd = 6.31 nM 8.20
CHEMBL304106 Kd = 10.0 nM 8.00
CHEMBL66441 Kd = 10.0 nM 8.00
CHEMBL68060 Kd = 10.0 nM 8.00
CHEMBL441252 Kd = 10.0 nM 8.00
CHEMBL57993 Kd = 10.0 nM 8.00
CHEMBL66332 Kd = 12.59 nM 7.90
CHEMBL67171 Kd = 12.59 nM 7.90
CHEMBL60504 Kd = 15.85 nM 7.80
CHEMBL66635 Kd = 19.95 nM 7.70