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Assay Detail

CHEMBL750065

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

Functional
Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuromedin-K receptor (CHEMBL4429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
Harrison T, Korsgaard MP, Swain CJ, Cascieri MA, Sadowski S, Seabrook GR.
Bioorg Med Chem Lett (1998) 8 : 1343 -1348
PubMed 9871763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.44 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437797 NEUROKININ B 1 8.22
CHEMBL106124 SENKTIDE 1 8.15
CHEMBL217406 NEUROKININ A 1 7.28
CHEMBL235363 SUBSTANCE P 1.0 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437797 NEUROKININ B EC50 = 6.0 nM 8.22
CHEMBL106124 SENKTIDE EC50 = 7.0 nM 8.15
CHEMBL217406 NEUROKININ A EC50 = 53.0 nM 7.28
CHEMBL235363 SUBSTANCE P EC50 = 793.0 nM 6.10