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Assay Detail

CHEMBL4042613

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Binding
Agonist activity at GPR35 in human HT-29 cells by DMR assay
ChEMBL ↗
42
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists.
Wei L, Wang J, Zhang X, Wang P, Zhao Y, Li J, Hou T, Qu L, Shi L, Liang X, Fang Y.
J Med Chem (2017) 60 : 362 -372
PubMed 27976894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 6.03 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100677 — — 2 8.24
CHEMBL4079816 — — 2 7.85
CHEMBL4082281 — — 2 7.29
CHEMBL4092954 — — 2 7.18
CHEMBL4081238 — — 2 6.82
CHEMBL4085211 — — 2 6.48
CHEMBL28079 ZAPRINAST 2.0 1 6.47
CHEMBL4066109 — — 2 6.24
CHEMBL4073902 — — 1 6.15
CHEMBL4105535 — — 2 6.05
CHEMBL4065291 — — 2 6.03
CHEMBL4103143 — — 2 5.85
CHEMBL1830823 — — 2 5.76
CHEMBL1600989 — — 1 5.70
CHEMBL4103860 — — 2 5.63
CHEMBL4084237 — — 1 5.58
CHEMBL4081445 — — 1 5.54
CHEMBL4096323 — — 1 5.37
CHEMBL4077503 — — 1 5.36
CHEMBL1765162 — — 1 5.17
CHEMBL4093683 — — 1 5.08
CHEMBL4078055 — — 1 5.07
CHEMBL4085935 — — 1 5.03
CHEMBL2333943 — — 1 4.97
CHEMBL1414071 — — 1 4.87
CHEMBL4062531 — — 1 4.83
CHEMBL4096105 — — 1 4.75
CHEMBL4088382 — — 1 4.67
CHEMBL83294 COUMARIN-3-CARBOXYLIC ACID — 1 4.04
CHEMBL1767304 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100677 — EC50 = 5.8 nM 8.24
CHEMBL4100677 — EC50 = 5.781 nM 8.24
CHEMBL4079816 — EC50 = 14.0 nM 7.85
CHEMBL4079816 — EC50 = 14.03 nM 7.85
CHEMBL4082281 — EC50 = 51.05 nM 7.29
CHEMBL4082281 — EC50 = 51.0 nM 7.29
CHEMBL4092954 — EC50 = 66.68 nM 7.18
CHEMBL4092954 — EC50 = 68.0 nM 7.17
CHEMBL4081238 — EC50 = 150.0 nM 6.82
CHEMBL4081238 — EC50 = 149.97 nM 6.82
CHEMBL4085211 — EC50 = 330.0 nM 6.48
CHEMBL4085211 — EC50 = 333.43 nM 6.48
CHEMBL28079 ZAPRINAST EC50 = 340.0 nM 6.47
CHEMBL4066109 — EC50 = 576.77 nM 6.24
CHEMBL4066109 — EC50 = 700.0 nM 6.16
CHEMBL4073902 — EC50 = 710.0 nM 6.15
CHEMBL4105535 — EC50 = 887.16 nM 6.05
CHEMBL4105535 — EC50 = 890.0 nM 6.05
CHEMBL4065291 — EC50 = 931.11 nM 6.03
CHEMBL4065291 — EC50 = 930.0 nM 6.03
CHEMBL4103143 — EC50 = 1410.0 nM 5.85
CHEMBL4103143 — EC50 = 1409.29 nM 5.85
CHEMBL1830823 — EC50 = 1750.0 nM 5.76
CHEMBL1830823 — EC50 = 1749.85 nM 5.76
CHEMBL1600989 — EC50 = 2020.0 nM 5.70
CHEMBL4103860 — EC50 = 2333.46 nM 5.63
CHEMBL4103860 — EC50 = 2330.0 nM 5.63
CHEMBL4084237 — EC50 = 2660.0 nM 5.58
CHEMBL4081445 — EC50 = 2910.0 nM 5.54
CHEMBL4096323 — EC50 = 4270.0 nM 5.37
CHEMBL4077503 — EC50 = 4340.0 nM 5.36
CHEMBL1765162 — EC50 = 6760.0 nM 5.17
CHEMBL4093683 — EC50 = 8220.0 nM 5.08
CHEMBL4078055 — EC50 = 8610.0 nM 5.07
CHEMBL4085935 — EC50 = 9270.0 nM 5.03
CHEMBL2333943 — EC50 = 10760.0 nM 4.97
CHEMBL1414071 — EC50 = 13520.0 nM 4.87
CHEMBL4062531 — EC50 = 14760.0 nM 4.83
CHEMBL4096105 — EC50 = 17700.0 nM 4.75
CHEMBL4088382 — EC50 = 21430.0 nM 4.67
CHEMBL83294 COUMARIN-3-CARBOXYLIC ACID EC50 = 92260.0 nM 4.04
CHEMBL1767304 — EC50 - — -