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Assay Detail

CHEMBL890161

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Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

SAR and QSAR studies on the N-terminally acylated pentapeptide agonists for GPR54.
Tomita K, Oishi S, Cluzeau J, Ohno H, Navenot JM, Wang ZX, Peiper SC, Akamatsu M, Fujii N.
J Med Chem (2007) 50 : 3222 -3228
PubMed 17579384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 8.72 9.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388586 1 9.16
CHEMBL268579 1 9.10
CHEMBL388146 1 9.00
CHEMBL226757 1 9.00
CHEMBL440431 1 9.00
CHEMBL223390 1 8.92
CHEMBL226566 1 8.92
CHEMBL388585 1 8.89
CHEMBL229621 1 8.85
CHEMBL226633 1 8.80
CHEMBL268660 1 8.77
CHEMBL227165 1 8.77
CHEMBL268659 1 8.77
CHEMBL226635 1 8.70
CHEMBL389708 1 8.68
CHEMBL229656 1 8.57
CHEMBL389493 1 8.52
CHEMBL387875 1 8.52
CHEMBL415004 1 8.52
CHEMBL226634 1 8.51
CHEMBL374398 1 8.51
CHEMBL387648 1 8.48
CHEMBL229655 1 8.48
CHEMBL387923 1 8.33
CHEMBL268661 1 8.30
CHEMBL274960 1 -
CHEMBL389262 1 -
CHEMBL226537 1 -
CHEMBL229103 1 -
CHEMBL415221 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388586 EC50 = 0.69 nM 9.16
CHEMBL268579 EC50 = 0.8 nM 9.10
CHEMBL388146 EC50 = 1.0 nM 9.00
CHEMBL226757 EC50 = 0.99 nM 9.00
CHEMBL440431 EC50 = 0.99 nM 9.00
CHEMBL223390 EC50 = 1.2 nM 8.92
CHEMBL226566 EC50 = 1.2 nM 8.92
CHEMBL388585 EC50 = 1.3 nM 8.89
CHEMBL229621 EC50 = 1.4 nM 8.85
CHEMBL226633 EC50 = 1.6 nM 8.80
CHEMBL268660 EC50 = 1.7 nM 8.77
CHEMBL227165 EC50 = 1.7 nM 8.77
CHEMBL268659 EC50 = 1.7 nM 8.77
CHEMBL226635 EC50 = 2.0 nM 8.70
CHEMBL389708 EC50 = 2.1 nM 8.68
CHEMBL229656 EC50 = 2.7 nM 8.57
CHEMBL389493 EC50 = 3.0 nM 8.52
CHEMBL387875 EC50 = 3.0 nM 8.52
CHEMBL415004 EC50 = 3.0 nM 8.52
CHEMBL226634 EC50 = 3.1 nM 8.51
CHEMBL374398 EC50 = 3.1 nM 8.51
CHEMBL387648 EC50 = 3.3 nM 8.48
CHEMBL229655 EC50 = 3.3 nM 8.48
CHEMBL387923 EC50 = 4.7 nM 8.33
CHEMBL268661 EC50 = 5.0 nM 8.30
CHEMBL274960 EC50 - -
CHEMBL389262 EC50 - -
CHEMBL226537 EC50 > 100.0 nM -
CHEMBL229103 EC50 - -
CHEMBL415221 EC50 > 100.0 nM -