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Assay Detail

CHEMBL3579719

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Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL ↗
67
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Probable G-protein coupled receptor 34 (CHEMBL3562165) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of lysophosphatidylserine analogs as agonists of G-protein-coupled receptors GPR34, P2Y10, and GPR174.
Ikubo M, Inoue A, Nakamura S, Jung S, Sayama M, Otani Y, Uwamizu A, Suzuki K, Kishi T, Shuto A, Ishiguro J, Okudaira M, Kano K, Makide K, Aoki J, Ohwada T.
J Med Chem (2015) 58 : 4204 -4219
PubMed 25970039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 67 6.18 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3577175 — — 2 6.80
CHEMBL3577174 — — 2 6.63
CHEMBL3577145 — — 2 6.54
CHEMBL3577140 — — 2 6.50
CHEMBL3577138 — — 2 6.39
CHEMBL3577171 — — 2 6.34
CHEMBL1742484 — — 2 6.26
CHEMBL3577151 — — 2 6.16
CHEMBL3577147 — — 2 6.08
CHEMBL3577182 — — 2 6.03
CHEMBL3577170 — — 2 6.03
CHEMBL3577144 — — 2 5.87
CHEMBL567724 — — 2 5.78
CHEMBL3577178 — — 2 5.75
CHEMBL3577149 — — 2 5.51
CHEMBL3577264 — — 1 -
CHEMBL3577263 — — 1 -
CHEMBL3577262 — — 1 -
CHEMBL3577181 — — 1 -
CHEMBL3577161 — — 1 -
CHEMBL3577179 — — 1 -
CHEMBL3577177 — — 1 -
CHEMBL3577176 — — 1 -
CHEMBL3577166 — — 1 -
CHEMBL3577167 — — 1 -
CHEMBL3577173 — — 1 -
CHEMBL3577172 — — 1 -
CHEMBL3577168 — — 1 -
CHEMBL3577169 — — 1 -
CHEMBL3577180 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3577175 — EC50 = 158.49 nM 6.80
CHEMBL3577175 — EC50 = 160.0 nM 6.80
CHEMBL3577174 — EC50 = 234.42 nM 6.63
CHEMBL3577174 — EC50 = 240.0 nM 6.62
CHEMBL3577145 — EC50 = 288.4 nM 6.54
CHEMBL3577145 — EC50 = 290.0 nM 6.54
CHEMBL3577140 — EC50 = 320.0 nM 6.50
CHEMBL3577140 — EC50 = 316.23 nM 6.50
CHEMBL3577138 — EC50 = 410.0 nM 6.39
CHEMBL3577138 — EC50 = 416.87 nM 6.38
CHEMBL3577171 — EC50 = 460.0 nM 6.34
CHEMBL3577171 — EC50 = 457.09 nM 6.34
CHEMBL1742484 — EC50 = 550.0 nM 6.26
CHEMBL1742484 — EC50 = 549.54 nM 6.26
CHEMBL3577151 — EC50 = 700.0 nM 6.16
CHEMBL3577151 — EC50 = 707.95 nM 6.15
CHEMBL3577147 — EC50 = 831.76 nM 6.08
CHEMBL3577147 — EC50 = 840.0 nM 6.08
CHEMBL3577182 — EC50 = 933.25 nM 6.03
CHEMBL3577170 — EC50 = 930.0 nM 6.03
CHEMBL3577182 — EC50 = 940.0 nM 6.03
CHEMBL3577170 — EC50 = 933.25 nM 6.03
CHEMBL3577144 — EC50 = 1348.96 nM 5.87
CHEMBL3577144 — EC50 = 1400.0 nM 5.85
CHEMBL567724 — EC50 = 1659.59 nM 5.78
CHEMBL567724 — EC50 = 1700.0 nM 5.77
CHEMBL3577178 — EC50 = 1800.0 nM 5.75
CHEMBL3577178 — EC50 = 1819.7 nM 5.74
CHEMBL3577149 — EC50 = 3100.0 nM 5.51
CHEMBL3577149 — EC50 = 3162.28 nM 5.50
CHEMBL3577153 — EC50 > 1000.0 nM -
CHEMBL3577152 — EC50 > 1000.0 nM -
CHEMBL3577150 — EC50 > 1000.0 nM -
CHEMBL3577148 — EC50 - — -
CHEMBL3577146 — EC50 > 1000.0 nM -
CHEMBL3577137 — EC50 > 1000.0 nM -
CHEMBL3577139 — EC50 > 1000.0 nM -
CHEMBL3577141 — EC50 > 1000.0 nM -
CHEMBL3577142 — EC50 > 1000.0 nM -
CHEMBL3577158 — EC50 - — -
CHEMBL3577176 — EC50 > 1000.0 nM -
CHEMBL3577168 — EC50 - — -
CHEMBL3577265 — EC50 - — -
CHEMBL3577177 — EC50 > 1000.0 nM -
CHEMBL3577179 — EC50 > 1000.0 nM -
CHEMBL3577180 — EC50 > 1000.0 nM -
CHEMBL3577181 — EC50 > 1000.0 nM -
CHEMBL3577262 — EC50 > 1000.0 nM -
CHEMBL3577263 — EC50 - — -
CHEMBL3577264 — EC50 - — -