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Assay Detail

CHEMBL814852

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Functional
Agonist activity at tachykinin receptor 2 in the rat colon muscularis mucosae
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Muscularis mucosa
Confidence 9 — Direct single protein target
Curated By Expert

Target

Substance-K receptor (CHEMBL4554)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potent and highly selective neurokinin antagonists.
Ward P, Ewan GB, Jordan CC, Ireland SJ, Hagan RM, Brown JR.
J Med Chem (1990) 33 : 1848 -1851
PubMed 1694545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.28 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301477 1 9.40
CHEMBL301841 1 9.40
CHEMBL235363 SUBSTANCE P 1.0 1 9.00
CHEMBL291903 1 8.57
CHEMBL54622 1 8.15
CHEMBL280020 1 8.08
CHEMBL2372949 1 7.96
CHEMBL299503 1 7.22
CHEMBL2372953 1 6.73
CHEMBL2372954 1 -
CHEMBL292435 1 -
CHEMBL293747 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301477 EC50 = 0.4 nM 9.40
CHEMBL301841 EC50 = 0.4 nM 9.40
CHEMBL235363 SUBSTANCE P EC50 = 1.0 nM 9.00
CHEMBL291903 EC50 = 2.7 nM 8.57
CHEMBL54622 EC50 = 7.1 nM 8.15
CHEMBL280020 EC50 = 8.3 nM 8.08
CHEMBL2372949 EC50 = 11.1 nM 7.96
CHEMBL299503 EC50 = 59.7 nM 7.22
CHEMBL2372953 EC50 = 188.0 nM 6.73
CHEMBL2372954 EC50 > 100.0 nM -
CHEMBL292435 EC50 > 500.0 nM -
CHEMBL293747 EC50 > 300.0 nM -