Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5505148

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

Functional
Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay
ChEMBL ↗
74
Total Activities
44
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Probable G-protein coupled receptor 132 (CHEMBL3085618) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Potent and Selective G2A (GPR132) Agonist.
Hernandez-Olmos V, Heering J, Marinescu B, Schermeng T, Ivanov VV, Moroz YS, Nevermann S, Mathes M, Ehrler JHM, Alnouri MW, Wolf M, Haydo AS, Schmachtel T, Zaliani A, Höfner G, Kaiser A, Schubert-Zsilavecz M, Beck-Sickinger AG, Offermanns S, Gribbon P, Rieger MA, Merk D, Sisignano M, Steinhilber D, Proschak E.
J Med Chem (2024) 67 : 10567 -10588
PubMed 38917049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 66 4.88 6.09
Activity 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5315640 — — 2 6.09
CHEMBL5549824 — — 2 5.76
CHEMBL5542713 — — 2 5.71
CHEMBL5558575 — — 2 5.54
CHEMBL5505872 — — 2 5.54
CHEMBL5532567 — — 2 5.48
CHEMBL5287669 — — 1 5.41
CHEMBL5558112 — — 2 5.21
CHEMBL5555854 — — 2 5.16
CHEMBL5558868 — — 2 5.14
CHEMBL5505940 — — 2 5.13
CHEMBL1077284 — — 1 5.12
CHEMBL5512528 — — 2 5.12
CHEMBL5556971 — — 2 5.06
CHEMBL5556769 — — 2 4.93
CHEMBL5555627 — — 2 4.92
CHEMBL5517738 — — 2 4.91
CHEMBL5527916 — — 2 4.88
CHEMBL5558798 — — 2 4.87
CHEMBL5558236 — — 2 4.73
CHEMBL5558889 — — 2 4.71
CHEMBL5532163 — — 2 4.56
CHEMBL5557073 — — 2 4.51
CHEMBL5512539 — — 2 4.42
CHEMBL5523620 — — 2 4.42
CHEMBL4297310 DORDAVIPRONE 3.0 1 4.41
CHEMBL5555495 — — 2 4.39
CHEMBL5558556 — — 2 4.30
CHEMBL5517769 — — 2 4.24
CHEMBL5559037 — — 2 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5315640 — EC50 = 812.83 nM 6.09
CHEMBL5315640 — EC50 = 820.0 nM 6.09
CHEMBL5549824 — EC50 = 1740.0 nM 5.76
CHEMBL5542713 — EC50 = 1949.84 nM 5.71
CHEMBL5542713 — EC50 = 1960.0 nM 5.71
CHEMBL5549824 — EC50 = 2511.89 nM 5.60
CHEMBL5505872 — EC50 = 2884.03 nM 5.54
CHEMBL5558575 — EC50 = 2884.03 nM 5.54
CHEMBL5505872 — EC50 = 2870.0 nM 5.54
CHEMBL5558575 — EC50 = 2920.0 nM 5.54
CHEMBL5532567 — EC50 = 3311.31 nM 5.48
CHEMBL5532567 — EC50 = 3340.0 nM 5.48
CHEMBL5287669 — EC50 = 3920.0 nM 5.41
CHEMBL5558112 — EC50 = 6200.0 nM 5.21
CHEMBL5558112 — EC50 = 6165.95 nM 5.21
CHEMBL5555854 — EC50 = 6918.31 nM 5.16
CHEMBL5555854 — EC50 = 6870.0 nM 5.16
CHEMBL5558868 — EC50 = 7244.36 nM 5.14
CHEMBL5505940 — EC50 = 7413.1 nM 5.13
CHEMBL5558868 — EC50 = 7330.0 nM 5.13
CHEMBL5512528 — EC50 = 7530.0 nM 5.12
CHEMBL5505940 — EC50 = 7500.0 nM 5.12
CHEMBL5512528 — EC50 = 7585.78 nM 5.12
CHEMBL1077284 — EC50 = 7500.0 nM 5.12
CHEMBL5556971 — EC50 = 8710.0 nM 5.06
CHEMBL5556971 — EC50 = 8709.64 nM 5.06
CHEMBL5556769 — EC50 = 11748.98 nM 4.93
CHEMBL5555627 — EC50 = 12000.0 nM 4.92
CHEMBL5555627 — EC50 = 11994.99 nM 4.92
CHEMBL5556769 — EC50 = 11900.0 nM 4.92
CHEMBL5517738 — EC50 = 12302.69 nM 4.91
CHEMBL5517738 — EC50 = 12200.0 nM 4.91
CHEMBL5527916 — EC50 = 13200.0 nM 4.88
CHEMBL5527916 — EC50 = 13182.57 nM 4.88
CHEMBL5558798 — EC50 = 13489.63 nM 4.87
CHEMBL5558798 — EC50 = 13500.0 nM 4.87
CHEMBL5558236 — EC50 = 18620.87 nM 4.73
CHEMBL5558236 — EC50 = 18700.0 nM 4.73
CHEMBL5558889 — EC50 = 19498.45 nM 4.71
CHEMBL5558889 — EC50 = 19600.0 nM 4.71
CHEMBL5532163 — EC50 = 27542.29 nM 4.56
CHEMBL5532163 — EC50 = 27500.0 nM 4.56
CHEMBL5557073 — EC50 = 31100.0 nM 4.51
CHEMBL5557073 — EC50 = 30902.95 nM 4.51
CHEMBL5512539 — EC50 = 38200.0 nM 4.42
CHEMBL5523620 — EC50 = 38018.94 nM 4.42
CHEMBL5523620 — EC50 = 38400.0 nM 4.42
CHEMBL5512539 — EC50 = 38018.94 nM 4.42
CHEMBL4297310 DORDAVIPRONE EC50 = 38600.0 nM 4.41
CHEMBL5555495 — EC50 = 40738.03 nM 4.39