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Assay Detail

CHEMBL4834976

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Functional
Agonist activity at human GPR35 receptor expressed in HT-29 cells assessed as reduction in dynamic mass redistribution response in presence of GPR35 antagonist ML-145 by DMR assay
ChEMBL ↗
36
Total Activities
36
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
IC50 36 6.35 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854346 — — 1 6.92
CHEMBL4077503 — — 1 6.89
CHEMBL4856916 — — 1 6.82
CHEMBL4847144 — — 1 6.80
CHEMBL4859764 — — 1 6.77
CHEMBL4870213 — — 1 6.75
CHEMBL4856069 — — 1 6.70
CHEMBL4865638 — — 1 6.68
CHEMBL4852667 — — 1 6.55
CHEMBL4850743 — — 1 6.54
CHEMBL4848109 — — 1 6.52
CHEMBL4875041 — — 1 6.48
CHEMBL4875009 — — 1 6.46
CHEMBL4862654 — — 1 6.46
CHEMBL4879017 — — 1 6.37
CHEMBL4861414 — — 1 6.36
CHEMBL4857772 — — 1 6.34
CHEMBL4853043 — — 1 6.33
CHEMBL4869539 — — 1 6.33
CHEMBL4856506 — — 1 6.33
CHEMBL4878979 — — 1 6.32
CHEMBL4871203 — — 1 6.32
CHEMBL4865971 — — 1 6.31
CHEMBL4848949 — — 1 6.27
CHEMBL1235421 PYRROLOQUINOLINE QUINONE — 1 6.24
CHEMBL4870255 — — 1 6.23
CHEMBL4847100 — — 1 6.21
CHEMBL4859675 — — 1 6.15
CHEMBL4875771 — — 1 6.10
CHEMBL3306990 — — 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854346 — IC50 = 120.0 nM 6.92
CHEMBL4077503 — IC50 = 130.0 nM 6.89
CHEMBL4856916 — IC50 = 150.0 nM 6.82
CHEMBL4847144 — IC50 = 160.0 nM 6.80
CHEMBL4859764 — IC50 = 170.0 nM 6.77
CHEMBL4870213 — IC50 = 180.0 nM 6.75
CHEMBL4856069 — IC50 = 200.0 nM 6.70
CHEMBL4865638 — IC50 = 210.0 nM 6.68
CHEMBL4852667 — IC50 = 282.0 nM 6.55
CHEMBL4850743 — IC50 = 290.0 nM 6.54
CHEMBL4848109 — IC50 = 300.0 nM 6.52
CHEMBL4875041 — IC50 = 330.0 nM 6.48
CHEMBL4875009 — IC50 = 350.0 nM 6.46
CHEMBL4862654 — IC50 = 350.0 nM 6.46
CHEMBL4879017 — IC50 = 430.0 nM 6.37
CHEMBL4861414 — IC50 = 440.0 nM 6.36
CHEMBL4857772 — IC50 = 460.0 nM 6.34
CHEMBL4856506 — IC50 = 470.0 nM 6.33
CHEMBL4869539 — IC50 = 470.0 nM 6.33
CHEMBL4853043 — IC50 = 470.0 nM 6.33
CHEMBL4878979 — IC50 = 480.0 nM 6.32
CHEMBL4871203 — IC50 = 480.0 nM 6.32
CHEMBL4865971 — IC50 = 494.0 nM 6.31
CHEMBL4848949 — IC50 = 540.0 nM 6.27
CHEMBL1235421 PYRROLOQUINOLINE QUINONE IC50 = 582.0 nM 6.24
CHEMBL4870255 — IC50 = 590.0 nM 6.23
CHEMBL4847100 — IC50 = 620.0 nM 6.21
CHEMBL4859675 — IC50 = 710.0 nM 6.15
CHEMBL4875771 — IC50 = 800.0 nM 6.10
CHEMBL3306990 — IC50 = 789.0 nM 6.10
CHEMBL4856029 — IC50 = 830.0 nM 6.08
CHEMBL4852718 — IC50 = 1030.0 nM 5.99
CHEMBL4872368 — IC50 = 1060.0 nM 5.97
CHEMBL4878047 — IC50 = 2260.0 nM 5.65
CHEMBL4860550 — IC50 = 2530.0 nM 5.60
CHEMBL4876009 — IC50 = 2529.0 nM 5.60