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Assay Detail

CHEMBL814855

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

Functional
In vitro agonistic activity against tachykinin receptor 2 of rat colon muscularis mucosae.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.
Deal MJ, Hagan RM, Ireland SJ, Jordan CC, McElroy AB, Porter B, Ross BC, Stephens-Smith M, Ward P.
J Med Chem (1992) 35 : 4195 -4204
PubMed 1331460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.09 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134091 1 8.89
CHEMBL217406 NEUROKININ A 1 8.77
CHEMBL335054 1 8.52
CHEMBL131872 1 8.43
CHEMBL134012 1 7.82
CHEMBL437797 NEUROKININ B 1 7.57
CHEMBL134481 1 7.48
CHEMBL267712 1 7.35
CHEMBL131923 1 7.23
CHEMBL135186 1 7.21
CHEMBL262048 1 7.04
CHEMBL335248 1 7.03
CHEMBL235363 SUBSTANCE P 1.0 1 6.78
CHEMBL339391 1 6.25
CHEMBL262049 1 5.92
CHEMBL337465 1 5.92
CHEMBL133362 1 5.86
CHEMBL337037 1 5.68
CHEMBL407511 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134091 EC50 = 1.3 nM 8.89
CHEMBL217406 NEUROKININ A EC50 = 1.7 nM 8.77
CHEMBL335054 EC50 = 3.0 nM 8.52
CHEMBL131872 EC50 = 3.7 nM 8.43
CHEMBL134012 EC50 = 15.0 nM 7.82
CHEMBL437797 NEUROKININ B EC50 = 27.0 nM 7.57
CHEMBL134481 EC50 = 33.0 nM 7.48
CHEMBL267712 EC50 = 45.0 nM 7.35
CHEMBL131923 EC50 = 59.0 nM 7.23
CHEMBL135186 EC50 = 62.0 nM 7.21
CHEMBL262048 EC50 = 92.0 nM 7.04
CHEMBL335248 EC50 = 94.0 nM 7.03
CHEMBL235363 SUBSTANCE P EC50 = 167.0 nM 6.78
CHEMBL339391 EC50 = 566.0 nM 6.25
CHEMBL262049 EC50 = 1190.0 nM 5.92
CHEMBL337465 EC50 = 1190.0 nM 5.92
CHEMBL133362 EC50 = 1390.0 nM 5.86
CHEMBL337037 EC50 = 2104.0 nM 5.68
CHEMBL407511 EC50 = 13000.0 nM 4.89