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Assay Detail

CHEMBL816681

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Functional
In vitro functional NK2 activity as inhibition of guinea pig bronchoconstriction
8
Total Activities
8
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 Expert

Target

Substance-K receptor (CHEMBL2647)
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 8 7.09 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305055 1 7.60
CHEMBL66106 1 7.30
CHEMBL66763 1 7.30
CHEMBL308891 1 7.30
CHEMBL446146 1 7.20
CHEMBL67508 1 7.00
CHEMBL303803 1 6.80
CHEMBL540651 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305055 Kd = 25.12 nM 7.60
CHEMBL66106 Kd = 50.12 nM 7.30
CHEMBL66763 Kd = 50.12 nM 7.30
CHEMBL308891 Kd = 50.12 nM 7.30
CHEMBL446146 Kd = 63.1 nM 7.20
CHEMBL67508 Kd = 100.0 nM 7.00
CHEMBL303803 Kd = 158.49 nM 6.80
CHEMBL540651 Kd = 630.96 nM 6.20