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Assay Detail

CHEMBL808517

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

Binding
Binding Affinity of [125I]-MePhe7-NKB towards Tachykinin receptor 3-CHO cell membranes(n=3-8)
7
Total Activities
7
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

2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.
Giardina GA, Sarau HM, Farina C, Medhurst AD, Grugni M, Foley JJ, Raveglia LF, Schmidt DB, Rigolio R, Vassallo M, Vecchietti V, Hay DW.
J Med Chem (1996) 39 : 2281 -2284
PubMed 8691422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.92 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10188 TALNETANT 2.0 1 9.00
CHEMBL346178 OSANETANT 2.0 1 8.92
CHEMBL10284 SB-222200 1 8.38
CHEMBL9643 1 7.88
CHEMBL9960 AZD-7624 2.0 1 7.75
CHEMBL429951 1 7.51
CHEMBL9843 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10188 TALNETANT Ki = 1.0 nM 9.00
CHEMBL346178 OSANETANT Ki = 1.2 nM 8.92
CHEMBL10284 SB-222200 Ki = 4.2 nM 8.38
CHEMBL9643 Ki = 13.3 nM 7.88
CHEMBL9960 AZD-7624 Ki = 18.0 nM 7.75
CHEMBL429951 Ki = 30.7 nM 7.51
CHEMBL9843 Ki = 925.0 nM 6.03