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Assay Detail

CHEMBL2155897

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Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

KiSS-1 receptor (CHEMBL5413)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
Asami T, Nishizawa N, Ishibashi Y, Nishibori K, Nakayama M, Horikoshi Y, Matsumoto S, Yamaguchi M, Matsumoto H, Tarui N, Ohtaki T, Kitada C.
Bioorg Med Chem Lett (2012) 22 : 6391 -6396
PubMed 22975302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 9.80 10.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151643 1 10.39
CHEMBL376756 KISSPEPTIN-10 3.0 1 10.31
CHEMBL2151646 1 10.30
CHEMBL2151642 1 10.19
CHEMBL2151654 1 10.14
CHEMBL2151653 1 10.01
CHEMBL2151650 1 10.00
CHEMBL2151652 1 9.96
CHEMBL2151649 1 9.89
CHEMBL2151648 1 9.62
CHEMBL2151651 1 9.62
CHEMBL2151655 1 9.23
CHEMBL2151644 1 9.21
CHEMBL2151647 1 9.14
CHEMBL2151645 1 9.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151643 EC50 = 0.041 nM 10.39
CHEMBL376756 KISSPEPTIN-10 EC50 = 0.049 nM 10.31
CHEMBL2151646 EC50 = 0.05 nM 10.30
CHEMBL2151642 EC50 = 0.065 nM 10.19
CHEMBL2151654 EC50 = 0.072 nM 10.14
CHEMBL2151653 EC50 = 0.098 nM 10.01
CHEMBL2151650 EC50 = 0.1 nM 10.00
CHEMBL2151652 EC50 = 0.11 nM 9.96
CHEMBL2151649 EC50 = 0.13 nM 9.89
CHEMBL2151648 EC50 = 0.24 nM 9.62
CHEMBL2151651 EC50 = 0.24 nM 9.62
CHEMBL2151655 EC50 = 0.59 nM 9.23
CHEMBL2151644 EC50 = 0.62 nM 9.21
CHEMBL2151647 EC50 = 0.73 nM 9.14
CHEMBL2151645 EC50 = 0.95 nM 9.02