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Assay Detail

CHEMBL5442696

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

Functional
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR35
39
Total Activities
38
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HTLA
Category GPCR beta-arrestin recruitment assay
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

EUbOPEN Chemogenomics Library - GPCR Dose-Respose
EUbOPEN
(2024)
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.51 6.68
EC50 1 6.35 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225963 PYRIDABEN 1 6.68
CHEMBL1384502 2 6.49
CHEMBL50588 EMETINE 4.0 1 6.45
CHEMBL1707 LOPERAMIDE HYDROCHLORIDE 4.0 1 6.35
CHEMBL256470 1 6.22
CHEMBL232656 BX 471 FREE BASE 2.0 1 5.97
CHEMBL1256876 1 5.50
CHEMBL1200776 CINACALCET HYDROCHLORIDE 4.0 1 5.47
CHEMBL1230609 FORETINIB 2.0 1 5.46
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE 4.0 1 5.46
CHEMBL4743495 1 5.44
CHEMBL487553 1 5.44
CHEMBL405355 NIGULDIPINE 2.0 1 5.43
CHEMBL1766103 1 5.41
CHEMBL59898 1 5.39
CHEMBL5089005 1 5.39
CHEMBL1474387 1 5.38
CHEMBL254760 1 5.37
CHEMBL4743049 1 5.36
CHEMBL531742 1 5.35
CHEMBL281350 SB-224289 1 5.34
CHEMBL2018875 1 5.33
CHEMBL5075931 1 5.28
CHEMBL259656 1 5.27
CHEMBL2111101 PIMAVANSERIN 4.0 1 5.25
CHEMBL567 PERPHENAZINE 4.0 1 5.22
CHEMBL103769 1 5.22
CHEMBL2181247 1 5.22
CHEMBL1471 APREPITANT 4.0 1 5.21
CHEMBL493982 VORAPAXAR 4.0 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225963 PYRIDABEN IC50 = 209.52 nM 6.68
CHEMBL1384502 IC50 = 323.69 nM 6.49
CHEMBL1384502 IC50 = 345.81 nM 6.46
CHEMBL50588 EMETINE IC50 = 352.52 nM 6.45
CHEMBL1707 LOPERAMIDE HYDROCHLORIDE EC50 = 444.0 nM 6.35
CHEMBL256470 IC50 = 608.24 nM 6.22
CHEMBL232656 BX 471 FREE BASE IC50 = 1069.98 nM 5.97
CHEMBL1256876 IC50 = 3155.17 nM 5.50
CHEMBL1200776 CINACALCET HYDROCHLORIDE IC50 = 3401.33 nM 5.47
CHEMBL1230609 FORETINIB IC50 = 3485.09 nM 5.46
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE IC50 = 3479.24 nM 5.46
CHEMBL4743495 IC50 = 3601.02 nM 5.44
CHEMBL487553 IC50 = 3633.11 nM 5.44
CHEMBL405355 NIGULDIPINE IC50 = 3743.05 nM 5.43
CHEMBL1766103 IC50 = 3929.62 nM 5.41
CHEMBL5089005 IC50 = 4056.81 nM 5.39
CHEMBL59898 IC50 = 4111.59 nM 5.39
CHEMBL1474387 IC50 = 4148.7 nM 5.38
CHEMBL254760 IC50 = 4246.68 nM 5.37
CHEMBL4743049 IC50 = 4418.81 nM 5.36
CHEMBL531742 IC50 = 4438.57 nM 5.35
CHEMBL281350 SB-224289 IC50 = 4581.88 nM 5.34
CHEMBL2018875 IC50 = 4655.95 nM 5.33
CHEMBL5075931 IC50 = 5214.15 nM 5.28
CHEMBL259656 IC50 = 5353.35 nM 5.27
CHEMBL2111101 PIMAVANSERIN IC50 = 5642.31 nM 5.25
CHEMBL567 PERPHENAZINE IC50 = 5966.8 nM 5.22
CHEMBL2181247 IC50 = 6014.75 nM 5.22
CHEMBL103769 IC50 = 6025.61 nM 5.22
CHEMBL1471 APREPITANT IC50 = 6238.53 nM 5.21
CHEMBL493982 VORAPAXAR IC50 = 7574.0 nM 5.12
CHEMBL3410223 IC50 = 7972.4 nM 5.10
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE IC50 = 8296.78 nM 5.08
CHEMBL23327 PURVALANOLA IC50 = 9784.77 nM 5.01
CHEMBL1200517 DIHYDROERGOTAMINE MESYLATE IC50 > 10000.0 nM -
CHEMBL535832 SEROTONIN HYDROCHLORIDE IC50 > 10000.0 nM -
CHEMBL45 MELATONIN IC50 > 10000.0 nM -
CHEMBL3215877 IC50 > 10000.0 nM -
CHEMBL9506 DEVAZEPIDE IC50 > 10000.0 nM -