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Assay Detail

CHEMBL1918727

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Functional
Agonist activity at GPR35 in human HT-29 cells after 1 hr by dynamic mass redistribution assay
19
Total Activities
19
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

Discovery of 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists.
Deng H, Hu H, He M, Hu J, Niu W, Ferrie AM, Fang Y.
J Med Chem (2011) 54 : 7385 -7396
PubMed 21950657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.44 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1914576 1 7.50
CHEMBL1914588 1 7.19
CHEMBL28079 ZAPRINAST 2.0 1 6.80
CHEMBL1914589 1 5.84
CHEMBL1914590 1 5.72
CHEMBL1914591 1 5.64
CHEMBL1914577 1 5.47
CHEMBL1914585 1 5.46
CHEMBL1914578 1 5.46
CHEMBL1914592 1 5.34
CHEMBL1914587 1 5.22
CHEMBL1914579 1 5.18
CHEMBL1914586 1 5.03
CHEMBL1914580 1 4.96
CHEMBL1914581 1 4.82
CHEMBL1914584 1 4.77
CHEMBL1173787 1 4.37
CHEMBL1914582 1 4.34
CHEMBL1914583 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1914576 EC50 = 32.0 nM 7.50
CHEMBL1914588 EC50 = 64.0 nM 7.19
CHEMBL28079 ZAPRINAST EC50 = 160.0 nM 6.80
CHEMBL1914589 EC50 = 1460.0 nM 5.84
CHEMBL1914590 EC50 = 1890.0 nM 5.72
CHEMBL1914591 EC50 = 2310.0 nM 5.64
CHEMBL1914577 EC50 = 3350.0 nM 5.47
CHEMBL1914585 EC50 = 3440.0 nM 5.46
CHEMBL1914578 EC50 = 3500.0 nM 5.46
CHEMBL1914592 EC50 = 4560.0 nM 5.34
CHEMBL1914587 EC50 = 6000.0 nM 5.22
CHEMBL1914579 EC50 = 6600.0 nM 5.18
CHEMBL1914586 EC50 = 9400.0 nM 5.03
CHEMBL1914580 EC50 = 11100.0 nM 4.96
CHEMBL1914581 EC50 = 15300.0 nM 4.82
CHEMBL1914584 EC50 = 17100.0 nM 4.77
CHEMBL1173787 EC50 = 42400.0 nM 4.37
CHEMBL1914582 EC50 = 45900.0 nM 4.34
CHEMBL1914583 EC50 = 53900.0 nM 4.27