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Assay Detail

CHEMBL4034862

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

Functional
Agonist activity at human GPR52 expressed in CHO cells assessed as increase in cAMP level after 30 mins by AlphaScreen assay
21
Total Activities
21
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

G-protein coupled receptor 52 (CHEMBL3297639)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and pharmacological evaluation of 4-azolyl-benzamide derivatives as novel GPR52 agonists.
Tokumaru K, Ito Y, Nomura I, Nakahata T, Shimizu Y, Kurimoto E, Aoyama K, Aso K.
Bioorg Med Chem (2017) 25 : 3098 -3115
PubMed 28433511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 6.79 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4059658 1 7.96
CHEMBL4087237 1 7.64
CHEMBL4075971 1 7.60
CHEMBL4101517 1 7.23
CHEMBL4080724 1 7.14
CHEMBL4082756 TP-024 1 7.12
CHEMBL4099668 1 7.08
CHEMBL4073584 1 6.96
CHEMBL4095110 1 6.89
CHEMBL4081439 1 6.80
CHEMBL4062229 1 6.77
CHEMBL4064577 1 6.68
CHEMBL4091030 1 6.66
CHEMBL4070849 1 6.58
CHEMBL4072782 1 6.43
CHEMBL4083957 1 6.42
CHEMBL4099457 1 6.40
CHEMBL4091718 1 6.16
CHEMBL4098770 1 5.85
CHEMBL4074656 1 5.41
CHEMBL4100408 TP-024n 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4059658 EC50 = 11.0 nM 7.96
CHEMBL4087237 EC50 = 23.0 nM 7.64
CHEMBL4075971 EC50 = 25.0 nM 7.60
CHEMBL4101517 EC50 = 59.0 nM 7.23
CHEMBL4080724 EC50 = 73.0 nM 7.14
CHEMBL4082756 TP-024 EC50 = 75.0 nM 7.12
CHEMBL4099668 EC50 = 83.0 nM 7.08
CHEMBL4073584 EC50 = 110.0 nM 6.96
CHEMBL4095110 EC50 = 130.0 nM 6.89
CHEMBL4081439 EC50 = 160.0 nM 6.80
CHEMBL4062229 EC50 = 170.0 nM 6.77
CHEMBL4064577 EC50 = 210.0 nM 6.68
CHEMBL4091030 EC50 = 220.0 nM 6.66
CHEMBL4070849 EC50 = 260.0 nM 6.58
CHEMBL4072782 EC50 = 370.0 nM 6.43
CHEMBL4083957 EC50 = 380.0 nM 6.42
CHEMBL4099457 EC50 = 400.0 nM 6.40
CHEMBL4091718 EC50 = 690.0 nM 6.16
CHEMBL4098770 EC50 = 1400.0 nM 5.85
CHEMBL4074656 EC50 = 3900.0 nM 5.41
CHEMBL4100408 TP-024n EC50 > 1000.0 nM -