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Assay Detail

CHEMBL811284

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Binding
Inhibitory activity against cloned human Tachykinin receptor 3 in CHO cells labeled with [125I][MePhe7]-NKB
5
Total Activities
5
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

Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
Boden P, Eden JM, Hodgson J, Horwell DC, Hughes J, McKnight AT, Lewthwaite RA, Pritchard MC, Raphy J, Meecham K, Ratcliffe GS, Suman-Chauhan N, Woodruff GN.
J Med Chem (1996) 39 : 1664 -1675
PubMed 8648606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.83 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45340 1 8.15
CHEMBL437797 NEUROKININ B 1 8.01
CHEMBL47146 1 7.80
CHEMBL444832 1 7.80
CHEMBL296014 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45340 IC50 = 7.0 nM 8.15
CHEMBL437797 NEUROKININ B IC50 = 9.7 nM 8.01
CHEMBL47146 IC50 = 16.0 nM 7.80
CHEMBL444832 IC50 = 16.0 nM 7.80
CHEMBL296014 IC50 = 40.0 nM 7.40