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Assay Detail

CHEMBL5134916

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Functional
Agonist activity at human GPR39 receptor expressed in CHO cells assessed as increase in ca2+ flux
20
Total Activities
17
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 Autocuration

Target

G-protein coupled receptor 39 (CHEMBL3091266)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators.
Burley R, Hewer RC, Teall M, Dickson L, Ossola B, Russell S, Bender C, Cheung T, Powell JAC, Xu X, Brice NL, Otter L, Arimont M, Kidd SL, Vidal D, Dale JW, Mervin L, Sore HF, Mateu N, Lakshminarayana N, Dawson LA, Carlton M, Bürli RW.
Bioorg Med Chem Lett (2022) 61 : 128607 -128607
PubMed 35123006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.28 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207240 1 8.52
CHEMBL3342358 1 7.82
CHEMBL5182651 1 7.82
CHEMBL5195894 1 7.80
CHEMBL5192920 1 7.77
CHEMBL5177479 2 7.77
CHEMBL5180126 1 7.20
CHEMBL5181574 1 7.11
CHEMBL5181167 2 7.10
CHEMBL5200611 1 6.32
CHEMBL3092413 1 5.20
CHEMBL5195424 1 -
CHEMBL5174704 1 -
CHEMBL5170821 2 -
CHEMBL5193472 1 -
CHEMBL5203229 1 -
CHEMBL5180932 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207240 EC50 = 3.0 nM 8.52
CHEMBL3342358 EC50 = 15.0 nM 7.82
CHEMBL5182651 EC50 = 15.0 nM 7.82
CHEMBL5195894 EC50 = 16.0 nM 7.80
CHEMBL5192920 EC50 = 17.0 nM 7.77
CHEMBL5177479 EC50 = 17.0 nM 7.77
CHEMBL5177479 EC50 = 26.0 nM 7.58
CHEMBL5180126 EC50 = 63.0 nM 7.20
CHEMBL5181574 EC50 = 78.0 nM 7.11
CHEMBL5181167 EC50 = 79.0 nM 7.10
CHEMBL5181167 EC50 = 240.0 nM 6.62
CHEMBL5200611 EC50 = 481.0 nM 6.32
CHEMBL3092413 EC50 = 6250.0 nM 5.20
CHEMBL5195424 EC50 > 31600.0 nM -
CHEMBL5174704 EC50 > 31600.0 nM -
CHEMBL5170821 EC50 > 10000.0 nM -
CHEMBL5170821 EC50 > 10000.0 nM -
CHEMBL5193472 EC50 > 50000.0 nM -
CHEMBL5203229 EC50 > 50000.0 nM -
CHEMBL5180932 EC50 > 50000.0 nM -