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Assay Detail

CHEMBL3300366

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Functional
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
32
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Hydroxycarboxylic acid receptor 2 (CHEMBL3785)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of (E)-2-(acrylamido)cyclohex-1-enecarboxylic acid derivatives as HCA1, HCA2, and HCA3 receptor agonists.
Bobileva O, Bokaldere R, Gailite V, Kaula I, Ikaunieks M, Duburs G, Petrovska R, Mandrika I, Klovins J, Loza E.
Bioorg Med Chem (2014) 22 : 3654 -3669
PubMed 24864041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Emax 16 - -
EC50 16 5.17 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3298702 2 6.05
CHEMBL3298701 2 5.85
CHEMBL482698 2 5.72
CHEMBL3299113 2 5.44
CHEMBL3299009 2 5.39
CHEMBL3297875 2 5.39
CHEMBL3298700 2 5.35
CHEMBL3299114 2 5.24
CHEMBL3299112 2 5.20
CHEMBL3299115 2 5.17
CHEMBL484719 2 5.08
CHEMBL3298703 2 4.90
CHEMBL3297797 2 4.58
CHEMBL3299016 2 4.56
CHEMBL3297874 2 4.44
CHEMBL3297876 2 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3298702 EC50 = 900.0 nM 6.05
CHEMBL3298701 EC50 = 1400.0 nM 5.85
CHEMBL482698 EC50 = 1900.0 nM 5.72
CHEMBL3299113 EC50 = 3600.0 nM 5.44
CHEMBL3297875 EC50 = 4100.0 nM 5.39
CHEMBL3299009 EC50 = 4100.0 nM 5.39
CHEMBL3298700 EC50 = 4500.0 nM 5.35
CHEMBL3299114 EC50 = 5800.0 nM 5.24
CHEMBL3299112 EC50 = 6300.0 nM 5.20
CHEMBL3299115 EC50 = 6800.0 nM 5.17
CHEMBL484719 EC50 = 8300.0 nM 5.08
CHEMBL3298703 EC50 = 12500.0 nM 4.90
CHEMBL3297797 EC50 = 26300.0 nM 4.58
CHEMBL3299016 EC50 = 27400.0 nM 4.56
CHEMBL3297874 EC50 = 36400.0 nM 4.44
CHEMBL3297876 EC50 = 51600.0 nM 4.29
CHEMBL3299112 Emax = 86.0 % -
CHEMBL3298701 Emax = 96.0 % -
CHEMBL3299113 Emax = 90.0 % -
CHEMBL3299114 Emax = 83.0 % -
CHEMBL3297875 Emax = 91.0 % -
CHEMBL3299016 Emax = 79.0 % -
CHEMBL484719 Emax = 97.0 % -
CHEMBL3299115 Emax = 93.0 % -
CHEMBL3297874 Emax = 82.0 % -
CHEMBL3299009 Emax = 99.0 % -
CHEMBL482698 Emax = 97.0 % -
CHEMBL3297797 Emax = 95.0 % -
CHEMBL3297876 Emax = 85.0 % -
CHEMBL3298700 Emax = 94.0 % -
CHEMBL3298702 Emax = 98.0 % -
CHEMBL3298703 Emax = 96.0 % -