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Assay Detail

CHEMBL4015220

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

Binding
Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay
63
Total Activities
63
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 84 (CHEMBL3714079)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diindolylmethane Derivatives: Potent Agonists of the Immunostimulatory Orphan G Protein-Coupled Receptor GPR84.
Pillaiyar T, Köse M, Sylvester K, Weighardt H, Thimm D, Borges G, Förster I, von Kügelgen I, Müller CE.
J Med Chem (2017) 60 : 3636 -3655
PubMed 28406627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 63 5.44 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221137 EMBELIN 1 6.40
CHEMBL4075099 1 5.97
CHEMBL246298 1 5.92
CHEMBL4101219 1 5.91
CHEMBL446452 ARUNDINE 3.0 1 5.79
CHEMBL4105236 1 5.64
CHEMBL4085470 1 5.53
CHEMBL4087204 1 5.53
CHEMBL4104992 1 5.40
CHEMBL4101728 1 5.36
CHEMBL4100658 1 5.27
CHEMBL4088884 1 5.26
CHEMBL4063898 1 5.22
CHEMBL107498 DECANOIC ACID 1 5.22
CHEMBL4062512 1 5.22
CHEMBL4095532 1 5.19
CHEMBL4099626 1 5.14
CHEMBL4082668 1 5.12
CHEMBL4078546 1 4.99
CHEMBL4087824 1 4.72
CHEMBL190134 1 -
CHEMBL2376559 1 -
CHEMBL4100585 1 -
CHEMBL4073783 1 -
CHEMBL522998 1 -
CHEMBL1995195 1 -
CHEMBL4066500 1 -
CHEMBL4077871 1 -
CHEMBL4103279 1 -
CHEMBL4085348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221137 EMBELIN EC50 = 400.0 nM 6.40
CHEMBL4075099 EC50 = 1080.0 nM 5.97
CHEMBL246298 EC50 = 1200.0 nM 5.92
CHEMBL4101219 EC50 = 1230.0 nM 5.91
CHEMBL446452 ARUNDINE EC50 = 1640.0 nM 5.79
CHEMBL4105236 EC50 = 2270.0 nM 5.64
CHEMBL4085470 EC50 = 2970.0 nM 5.53
CHEMBL4087204 EC50 = 2970.0 nM 5.53
CHEMBL4104992 EC50 = 3980.0 nM 5.40
CHEMBL4101728 EC50 = 4330.0 nM 5.36
CHEMBL4100658 EC50 = 5340.0 nM 5.27
CHEMBL4088884 EC50 = 5470.0 nM 5.26
CHEMBL4063898 EC50 = 6070.0 nM 5.22
CHEMBL107498 DECANOIC ACID EC50 = 6080.0 nM 5.22
CHEMBL4062512 EC50 = 6070.0 nM 5.22
CHEMBL4095532 EC50 = 6470.0 nM 5.19
CHEMBL4099626 EC50 = 7290.0 nM 5.14
CHEMBL4082668 EC50 = 7530.0 nM 5.12
CHEMBL4078546 EC50 = 10300.0 nM 4.99
CHEMBL4087824 EC50 = 19000.0 nM 4.72
CHEMBL4059692 EC50 > 10000.0 nM -
CHEMBL4095700 EC50 - -
CHEMBL4068351 EC50 - -
CHEMBL4103460 EC50 - -
CHEMBL4079202 EC50 - -
CHEMBL4093996 EC50 >= 10000.0 nM -
CHEMBL246504 EC50 - -
CHEMBL397514 EC50 > 10000.0 nM -
CHEMBL4071153 EC50 - -
CHEMBL4059770 EC50 - -
CHEMBL4081701 EC50 - -
CHEMBL4100764 EC50 - -
CHEMBL4090496 EC50 - -
CHEMBL578425 EC50 - -
CHEMBL4087145 EC50 - -
CHEMBL4087988 EC50 > 10000.0 nM -
CHEMBL1914909 EC50 - -
CHEMBL4074055 EC50 - -
CHEMBL4093108 EC50 - -
CHEMBL2376692 EC50 - -
CHEMBL4085348 EC50 - -
CHEMBL4103279 EC50 - -
CHEMBL4077871 EC50 > 10000.0 nM -
CHEMBL4066500 EC50 > 10000.0 nM -
CHEMBL1995195 EC50 - -
CHEMBL522998 EC50 > 10000.0 nM -
CHEMBL4073783 EC50 > 10000.0 nM -
CHEMBL4100585 EC50 - -
CHEMBL2376559 EC50 - -
CHEMBL190134 EC50 > 10000.0 nM -