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Assay Detail

CHEMBL811276

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

Binding
Binding affinity towards human Tachykinin receptor 3 stably expressed in CHO cells using [125I][MePhe7]-NKB as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists
Boden P, Eden J, Hodgson J, Horwell D, Pritchard M, Raphy J, Suman-Chauhan N
Bioorg Med Chem Lett (1995) 5 : 1773 -1778
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.47 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45340 1 8.14
CHEMBL437797 NEUROKININ B 1 8.00
CHEMBL47146 1 7.80
CHEMBL106124 SENKTIDE 1 7.68
CHEMBL444832 1 7.40
CHEMBL44965 1 7.37
CHEMBL47641 1 7.28
CHEMBL44686 1 7.13
CHEMBL296983 1 6.46
CHEMBL45278 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45340 IC50 = 7.3 nM 8.14
CHEMBL437797 NEUROKININ B IC50 = 10.0 nM 8.00
CHEMBL47146 IC50 = 16.0 nM 7.80
CHEMBL106124 SENKTIDE IC50 = 21.0 nM 7.68
CHEMBL444832 IC50 = 40.0 nM 7.40
CHEMBL44965 IC50 = 43.0 nM 7.37
CHEMBL47641 IC50 = 52.0 nM 7.28
CHEMBL44686 IC50 = 74.0 nM 7.13
CHEMBL296983 IC50 = 350.0 nM 6.46
CHEMBL45278 IC50 > 10000.0 nM -