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Assay Detail

CHEMBL3373359

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Binding
Agonist activity at human NK3R expressed in CHO cells assessed as potentiation of senktide-induced effect
6
Total Activities
6
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 Autocuration

Target

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

Publication

Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
Misu R, Oishi S, Yamada A, Yamamura T, Matsuda F, Yamamoto K, Noguchi T, Ohno H, Okamura H, Ohkura S, Fujii N.
J Med Chem (2014) 57 : 8646 -8651
PubMed 25247671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.83 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106124 SENKTIDE 1 7.96
CHEMBL3361404 1 7.80
CHEMBL3361408 1 7.00
CHEMBL3361407 1 6.43
CHEMBL3361405 1 6.04
CHEMBL3361406 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106124 SENKTIDE EC50 = 11.0 nM 7.96
CHEMBL3361404 EC50 = 16.0 nM 7.80
CHEMBL3361408 EC50 = 100.0 nM 7.00
CHEMBL3361407 EC50 = 370.0 nM 6.43
CHEMBL3361405 EC50 = 920.0 nM 6.04
CHEMBL3361406 EC50 = 1900.0 nM 5.72