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Assay Detail

CHEMBL811317

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro binding to Tachykinin receptor 2
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
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
Ki 20 9.13 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67171 1 9.70
CHEMBL304106 1 9.52
CHEMBL66441 1 9.52
CHEMBL441252 1 9.52
CHEMBL66635 1 9.52
CHEMBL66332 1 9.40
CHEMBL60504 1 9.40
CHEMBL68234 1 9.22
CHEMBL303803 1 9.15
CHEMBL68060 2 9.10
CHEMBL302329 1 9.10
CHEMBL57993 1 9.05
CHEMBL446146 1 9.00
CHEMBL66763 1 9.00
CHEMBL540651 1 8.70
CHEMBL308891 1 8.70
CHEMBL305055 1 8.70
CHEMBL66106 1 8.70
CHEMBL67508 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67171 Ki = 0.2 nM 9.70
CHEMBL304106 Ki = 0.3 nM 9.52
CHEMBL66441 Ki = 0.3 nM 9.52
CHEMBL441252 Ki = 0.3 nM 9.52
CHEMBL66635 Ki = 0.3 nM 9.52
CHEMBL66332 Ki = 0.4 nM 9.40
CHEMBL60504 Ki = 0.4 nM 9.40
CHEMBL68234 Ki = 0.6 nM 9.22
CHEMBL303803 Ki = 0.7 nM 9.15
CHEMBL302329 Ki = 0.8 nM 9.10
CHEMBL68060 Ki = 0.8 nM 9.10
CHEMBL57993 Ki = 0.9 nM 9.05
CHEMBL446146 Ki = 1.0 nM 9.00
CHEMBL66763 Ki = 1.0 nM 9.00
CHEMBL68060 Ki = 1.0 nM 9.00
CHEMBL540651 Ki = 2.0 nM 8.70
CHEMBL308891 Ki = 2.0 nM 8.70
CHEMBL305055 Ki = 2.0 nM 8.70
CHEMBL66106 Ki = 2.0 nM 8.70
CHEMBL67508 Ki = 3.0 nM 8.52