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Assay Detail

CHEMBL5385083

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

Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response incubated for 10 mins by calcium mobilization assay
44
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 84 (CHEMBL3714079)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Unsymmetrical Phosphodiesters as GPR84 Antagonists with High Blood Exposure for the Treatment of Lung Inflammation.
Li SX, Wang SW, Chen LH, Zhang Q, Lu D, Chen J, Fang YC, Gu M, Xie X, Nan FJ.
J Med Chem (2023) 66 : 5820 -5838
PubMed 37053384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 6.34 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5413740 1 7.92
CHEMBL5411648 1 7.82
CHEMBL5433078 1 7.64
CHEMBL5395660 2 7.60
CHEMBL5428552 1 7.39
CHEMBL5416118 1 7.21
CHEMBL5400040 1 7.17
CHEMBL5194984 1 7.13
CHEMBL5407283 1 7.04
CHEMBL5429540 1 6.97
CHEMBL5394910 1 6.96
CHEMBL5423643 1 6.90
CHEMBL5417993 1 6.89
CHEMBL5434490 1 6.78
CHEMBL5396626 1 6.71
CHEMBL5421575 1 6.71
CHEMBL5420273 1 6.66
CHEMBL5395766 1 6.62
CHEMBL5407593 1 6.49
CHEMBL5431524 1 6.47
CHEMBL5425683 1 6.40
CHEMBL5433203 1 6.39
CHEMBL5402662 1 6.35
CHEMBL5439033 1 6.29
CHEMBL5412502 1 6.26
CHEMBL5404018 1 6.26
CHEMBL5418028 1 6.21
CHEMBL5400422 1 6.18
CHEMBL5413350 1 6.15
CHEMBL5404966 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5413740 IC50 = 12.0 nM 7.92
CHEMBL5411648 IC50 = 15.0 nM 7.82
CHEMBL5433078 IC50 = 23.0 nM 7.64
CHEMBL5395660 IC50 = 25.0 nM 7.60
CHEMBL5428552 IC50 = 41.0 nM 7.39
CHEMBL5416118 IC50 = 62.0 nM 7.21
CHEMBL5400040 IC50 = 68.0 nM 7.17
CHEMBL5395660 IC50 = 69.0 nM 7.16
CHEMBL5194984 IC50 = 74.0 nM 7.13
CHEMBL5407283 IC50 = 91.0 nM 7.04
CHEMBL5429540 IC50 = 108.0 nM 6.97
CHEMBL5394910 IC50 = 110.0 nM 6.96
CHEMBL5423643 IC50 = 126.0 nM 6.90
CHEMBL5417993 IC50 = 130.0 nM 6.89
CHEMBL5434490 IC50 = 166.0 nM 6.78
CHEMBL5421575 IC50 = 196.0 nM 6.71
CHEMBL5396626 IC50 = 194.0 nM 6.71
CHEMBL5420273 IC50 = 219.0 nM 6.66
CHEMBL5395766 IC50 = 238.0 nM 6.62
CHEMBL5407593 IC50 = 325.0 nM 6.49
CHEMBL5431524 IC50 = 340.0 nM 6.47
CHEMBL5425683 IC50 = 396.0 nM 6.40
CHEMBL5433203 IC50 = 405.0 nM 6.39
CHEMBL5402662 IC50 = 450.0 nM 6.35
CHEMBL5439033 IC50 = 517.0 nM 6.29
CHEMBL5412502 IC50 = 554.0 nM 6.26
CHEMBL5404018 IC50 = 547.0 nM 6.26
CHEMBL5418028 IC50 = 609.0 nM 6.21
CHEMBL5400422 IC50 = 658.0 nM 6.18
CHEMBL5413350 IC50 = 711.0 nM 6.15
CHEMBL5404966 IC50 = 817.0 nM 6.09
CHEMBL5409696 IC50 = 1280.0 nM 5.89
CHEMBL5394273 IC50 = 1730.0 nM 5.76
CHEMBL5394851 IC50 = 2120.0 nM 5.67
CHEMBL5437225 IC50 = 2830.0 nM 5.55
CHEMBL5415068 IC50 = 2980.0 nM 5.53
CHEMBL5414181 IC50 = 3840.0 nM 5.42
CHEMBL5423506 IC50 = 4010.0 nM 5.40
CHEMBL5404335 IC50 = 3990.0 nM 5.40
CHEMBL5395990 IC50 = 6300.0 nM 5.20
CHEMBL5418832 IC50 = 13200.0 nM 4.88
CHEMBL5433983 IC50 = 21800.0 nM 4.66
CHEMBL5425199 IC50 = 29600.0 nM 4.53
CHEMBL5434645 IC50 = 39500.0 nM 4.40