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Assay Detail

CHEMBL5368565

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Functional
Agonist activity at human GPR55 expressed in human HEK293 cells assessed as effect on calcium flux incubated for 5 mins by FLIPR analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 55 (CHEMBL1075322)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of Novel CNS-Penetrant GPR55 Agonists.
Hewer RC, Christie LA, Doyle KJ, Xu X, Roberts MJ, Dickson L, Cheung T, Cadwalladr DH, Pickford P, Teall M, Powell JAC, Sheardown S, Narayana L, Brice NL, Dawson LA, Carlton M, Bürli RW.
J Med Chem (2023) 66 : 12858 -12876
PubMed 37708305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 6.94 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5414688 1 9.64
CHEMBL5428306 1 9.62
CHEMBL5426486 1 9.36
CHEMBL5439124 1 8.52
CHEMBL5427885 1 8.43
CHEMBL5428424 1 7.99
CHEMBL5424329 1 7.86
CHEMBL5409272 1 7.46
CHEMBL5415218 1 7.36
CHEMBL5430516 1 7.26
CHEMBL5428111 1 7.10
CHEMBL5416405 1 7.07
CHEMBL5402444 1 6.96
CHEMBL5404659 1 6.88
CHEMBL5419220 1 6.37
CHEMBL5411638 1 6.25
CHEMBL5403436 1 6.24
CHEMBL5429149 1 6.08
CHEMBL5395169 1 6.03
CHEMBL5412330 1 5.83
CHEMBL5415436 1 5.79
CHEMBL5432182 1 5.76
CHEMBL5425510 1 5.75
CHEMBL5429074 1 5.71
CHEMBL5436151 1 5.43
CHEMBL5433646 1 5.34
CHEMBL5414902 1 5.33
CHEMBL5434243 1 -
CHEMBL5440591 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5414688 EC50 = 0.227 nM 9.64
CHEMBL5428306 EC50 = 0.239 nM 9.62
CHEMBL5426486 EC50 = 0.439 nM 9.36
CHEMBL5439124 EC50 = 3.01 nM 8.52
CHEMBL5427885 EC50 = 3.76 nM 8.43
CHEMBL5428424 EC50 = 10.2 nM 7.99
CHEMBL5424329 EC50 = 13.8 nM 7.86
CHEMBL5409272 EC50 = 34.4 nM 7.46
CHEMBL5415218 EC50 = 43.7 nM 7.36
CHEMBL5430516 EC50 = 54.7 nM 7.26
CHEMBL5428111 EC50 = 79.6 nM 7.10
CHEMBL5416405 EC50 = 85.1 nM 7.07
CHEMBL5402444 EC50 = 111.0 nM 6.96
CHEMBL5404659 EC50 = 131.0 nM 6.88
CHEMBL5419220 EC50 = 427.0 nM 6.37
CHEMBL5411638 EC50 = 567.0 nM 6.25
CHEMBL5403436 EC50 = 573.0 nM 6.24
CHEMBL5429149 EC50 = 830.0 nM 6.08
CHEMBL5395169 EC50 = 927.0 nM 6.03
CHEMBL5412330 EC50 = 1490.0 nM 5.83
CHEMBL5415436 EC50 = 1620.0 nM 5.79
CHEMBL5432182 EC50 = 1730.0 nM 5.76
CHEMBL5425510 EC50 = 1790.0 nM 5.75
CHEMBL5429074 EC50 = 1950.0 nM 5.71
CHEMBL5436151 EC50 = 3680.0 nM 5.43
CHEMBL5433646 EC50 = 4570.0 nM 5.34
CHEMBL5414902 EC50 = 4690.0 nM 5.33
CHEMBL5434243 EC50 > 10000.0 nM -
CHEMBL5440591 EC50 > 10000.0 nM -