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Assay Detail

CHEMBL750067

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

Binding
Compound was evaluated for its ability to displace [3H]NKB binding in hNK3 receptors expressed in CHO cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
IC50 4 7.94 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106124 SENKTIDE 1 9.00
CHEMBL437797 NEUROKININ B 1 8.52
CHEMBL217406 NEUROKININ A 1 7.35
CHEMBL235363 SUBSTANCE P 1.0 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106124 SENKTIDE IC50 = 1.0 nM 9.00
CHEMBL437797 NEUROKININ B IC50 = 3.0 nM 8.52
CHEMBL217406 NEUROKININ A IC50 = 45.0 nM 7.35
CHEMBL235363 SUBSTANCE P IC50 = 125.0 nM 6.90