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Assay Detail

CHEMBL5259642

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Competitive binding affinity to Nluc-fused human GPR35 expressed in CHO-K1 cells assessed as inhibition constant using furimazine as substrate incubated for 30 mins followed by substrate addition by in presence of 10-(4-(2-(4-(4-((2,8-dicarboxy-6-hydroxy-10-methylpyrido[3,2-g]quinolin-4-yl)oxy)butyl)-1H-1,2,3-triazol-1-yl)ethoxy)phenyl)-5,5-difluoro-2,7,9-trimethyl-5H-imidazo[1,2-c]pyrrolo[2,1-f][1,3,2]diazaborinin-6-ium-5-uide
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development and Characterization of Fluorescent Probes for the G Protein-Coupled Receptor 35.
Wei L, Xiang K, Kang H, Yu Y, Fan H, Zhou H, Hou T, Ge Y, Wang J, Guo Z, Chen Y, Zhao Y, Liang X.
ACS Med Chem Lett (2023) 14 : 411 -416
PubMed 37077394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.13 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1384502 1 8.40
CHEMBL3306990 1 8.22
CHEMBL4175848 1 8.00
CHEMBL177880 PAMOIC ACID 1 7.64
CHEMBL4878979 1 7.55
CHEMBL4100677 1 7.29
CHEMBL1708510 1 6.63
CHEMBL1235421 PYRROLOQUINOLINE QUINONE 1 6.48
CHEMBL4081238 1 6.45
CHEMBL28079 ZAPRINAST 2.0 1 6.21
CHEMBL428880 CROMOLYN 4.0 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1384502 Ki = 4.0 nM 8.40
CHEMBL3306990 Ki = 6.0 nM 8.22
CHEMBL4175848 Ki = 10.0 nM 8.00
CHEMBL177880 PAMOIC ACID Ki = 23.0 nM 7.64
CHEMBL4878979 Ki = 28.0 nM 7.55
CHEMBL4100677 Ki = 51.0 nM 7.29
CHEMBL1708510 Ki = 236.0 nM 6.63
CHEMBL1235421 PYRROLOQUINOLINE QUINONE Ki = 332.0 nM 6.48
CHEMBL4081238 Ki = 352.0 nM 6.45
CHEMBL28079 ZAPRINAST Ki = 612.0 nM 6.21
CHEMBL428880 CROMOLYN Ki = 2970.0 nM 5.53