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Assay Detail

CHEMBL4834974

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Functional
Agonist activity at human GPR35 receptor expressed in HT-29 cells assessed as dynamic mass redistribution response by DMR assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 35 (CHEMBL1293267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationship Studies of Coumarin-like Diacid Derivatives as Human G Protein-Coupled Receptor-35 (hGPR35) Agonists and a Consequent New Design Principle.
Wei L, Hou T, Li J, Zhang X, Zhou H, Wang Z, Cheng J, Xiang K, Wang J, Zhao Y, Liang X.
J Med Chem (2021) 64 : 2634 -2647
PubMed 33630609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 6.78 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3306990 1 8.10
CHEMBL4848109 1 7.89
CHEMBL4859764 1 7.82
CHEMBL4857772 1 7.77
CHEMBL4870213 1 7.77
CHEMBL4869539 1 7.77
CHEMBL4856029 1 7.75
CHEMBL4856506 1 7.70
CHEMBL4861414 1 7.66
CHEMBL4850743 1 7.60
CHEMBL4852718 1 7.48
CHEMBL4865638 1 7.43
CHEMBL4865971 1 7.37
CHEMBL4848949 1 7.35
CHEMBL4856069 1 7.32
CHEMBL4876009 1 7.27
CHEMBL4871203 1 7.19
CHEMBL1235421 PYRROLOQUINOLINE QUINONE 1 7.15
CHEMBL4878979 1 7.08
CHEMBL4875009 1 7.04
CHEMBL4847100 1 7.04
CHEMBL4852667 1 7.00
CHEMBL4862654 1 6.85
CHEMBL4879017 1 6.51
CHEMBL28079 ZAPRINAST 2.0 1 6.47
CHEMBL4870255 1 6.41
CHEMBL4878047 1 5.80
CHEMBL4875771 1 5.74
CHEMBL4853043 1 5.68
CHEMBL4859675 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3306990 EC50 = 8.0 nM 8.10
CHEMBL4848109 EC50 = 13.0 nM 7.89
CHEMBL4859764 EC50 = 15.0 nM 7.82
CHEMBL4857772 EC50 = 17.0 nM 7.77
CHEMBL4870213 EC50 = 17.0 nM 7.77
CHEMBL4869539 EC50 = 17.0 nM 7.77
CHEMBL4856029 EC50 = 18.0 nM 7.75
CHEMBL4856506 EC50 = 20.0 nM 7.70
CHEMBL4861414 EC50 = 22.0 nM 7.66
CHEMBL4850743 EC50 = 25.0 nM 7.60
CHEMBL4852718 EC50 = 33.0 nM 7.48
CHEMBL4865638 EC50 = 37.0 nM 7.43
CHEMBL4865971 EC50 = 43.0 nM 7.37
CHEMBL4848949 EC50 = 45.0 nM 7.35
CHEMBL4856069 EC50 = 48.0 nM 7.32
CHEMBL4876009 EC50 = 54.0 nM 7.27
CHEMBL4871203 EC50 = 65.0 nM 7.19
CHEMBL1235421 PYRROLOQUINOLINE QUINONE EC50 = 71.0 nM 7.15
CHEMBL4878979 EC50 = 83.0 nM 7.08
CHEMBL4847100 EC50 = 92.0 nM 7.04
CHEMBL4875009 EC50 = 92.0 nM 7.04
CHEMBL4852667 EC50 = 100.0 nM 7.00
CHEMBL4862654 EC50 = 140.0 nM 6.85
CHEMBL4879017 EC50 = 310.0 nM 6.51
CHEMBL28079 ZAPRINAST EC50 = 340.0 nM 6.47
CHEMBL4870255 EC50 = 390.0 nM 6.41
CHEMBL4878047 EC50 = 1600.0 nM 5.80
CHEMBL4875771 EC50 = 1840.0 nM 5.74
CHEMBL4853043 EC50 = 2070.0 nM 5.68
CHEMBL4859675 EC50 = 2180.0 nM 5.66
CHEMBL4856916 EC50 = 2330.0 nM 5.63
CHEMBL4875041 EC50 = 2740.0 nM 5.56
CHEMBL4847144 EC50 = 2880.0 nM 5.54
CHEMBL4860550 EC50 = 2920.0 nM 5.54
CHEMBL4077503 EC50 = 4340.0 nM 5.36
CHEMBL4872368 EC50 = 8630.0 nM 5.06
CHEMBL4854346 EC50 = 23930.0 nM 4.62