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Assay Detail

CHEMBL4014236

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Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL ↗
72
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Probable G-protein coupled receptor 34 (CHEMBL1075291) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Probing the Hydrophobic Binding Pocket of G-Protein-Coupled Lysophosphatidylserine Receptor GPR34/LPS1 by Docking-Aided Structure-Activity Analysis.
Sayama M, Inoue A, Nakamura S, Jung S, Ikubo M, Otani Y, Uwamizu A, Kishi T, Makide K, Aoki J, Hirokawa T, Ohwada T.
J Med Chem (2017) 60 : 6384 -6399
PubMed 28715213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 72 6.65 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062945 — — 2 8.10
CHEMBL4095241 — — 2 7.85
CHEMBL4098603 — — 2 7.75
CHEMBL4096239 — — 2 7.41
CHEMBL4090880 — — 2 7.35
CHEMBL4071570 — — 2 7.31
CHEMBL4067822 — — 2 7.11
CHEMBL4090455 — — 2 7.09
CHEMBL4100630 — — 2 7.00
CHEMBL4098171 — — 2 6.98
CHEMBL4071116 — — 2 6.94
CHEMBL4062480 — — 2 6.93
CHEMBL4059731 — — 2 6.77
CHEMBL4082629 — — 2 6.75
CHEMBL3814092 — — 2 6.75
CHEMBL4068868 — — 2 6.68
CHEMBL4072692 — — 2 6.66
CHEMBL4067351 — — 2 6.59
CHEMBL1742484 — — 2 6.38
CHEMBL4068969 — — 2 6.26
CHEMBL4084094 — — 2 6.19
CHEMBL4102082 — — 2 6.10
CHEMBL4089962 — — 2 6.05
CHEMBL4061305 — — 2 5.92
CHEMBL4081667 — — 2 5.92
CHEMBL4091854 — — 2 5.89
CHEMBL3577179 — — 2 5.80
CHEMBL4083168 — — 2 5.77
CHEMBL4094801 — — 2 5.71
CHEMBL4060207 — — 2 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062945 — EC50 = 7.943 nM 8.10
CHEMBL4062945 — EC50 = 7.9 nM 8.10
CHEMBL4095241 — EC50 = 14.0 nM 7.85
CHEMBL4095241 — EC50 = 14.45 nM 7.84
CHEMBL4098603 — EC50 = 18.0 nM 7.75
CHEMBL4098603 — EC50 = 17.78 nM 7.75
CHEMBL4096239 — EC50 = 39.0 nM 7.41
CHEMBL4096239 — EC50 = 38.9 nM 7.41
CHEMBL4090880 — EC50 = 45.0 nM 7.35
CHEMBL4090880 — EC50 = 45.71 nM 7.34
CHEMBL4071570 — EC50 = 49.0 nM 7.31
CHEMBL4071570 — EC50 = 48.98 nM 7.31
CHEMBL4067822 — EC50 = 77.62 nM 7.11
CHEMBL4067822 — EC50 = 78.0 nM 7.11
CHEMBL4090455 — EC50 = 82.0 nM 7.09
CHEMBL4090455 — EC50 = 81.28 nM 7.09
CHEMBL4100630 — EC50 = 100.0 nM 7.00
CHEMBL4100630 — EC50 = 102.33 nM 6.99
CHEMBL4098171 — EC50 = 104.71 nM 6.98
CHEMBL4098171 — EC50 = 110.0 nM 6.96
CHEMBL4071116 — EC50 = 114.82 nM 6.94
CHEMBL4062480 — EC50 = 117.49 nM 6.93
CHEMBL4071116 — EC50 = 120.0 nM 6.92
CHEMBL4062480 — EC50 = 120.0 nM 6.92
CHEMBL4059731 — EC50 = 169.82 nM 6.77
CHEMBL4059731 — EC50 = 170.0 nM 6.77
CHEMBL3814092 — EC50 = 180.0 nM 6.75
CHEMBL4082629 — EC50 = 180.0 nM 6.75
CHEMBL4082629 — EC50 = 177.83 nM 6.75
CHEMBL3814092 — EC50 = 181.97 nM 6.74
CHEMBL4068868 — EC50 = 210.0 nM 6.68
CHEMBL4068868 — EC50 = 213.8 nM 6.67
CHEMBL4072692 — EC50 = 220.0 nM 6.66
CHEMBL4072692 — EC50 = 218.78 nM 6.66
CHEMBL4067351 — EC50 = 257.04 nM 6.59
CHEMBL4067351 — EC50 = 260.0 nM 6.58
CHEMBL1742484 — EC50 = 420.0 nM 6.38
CHEMBL1742484 — EC50 = 416.87 nM 6.38
CHEMBL4068969 — EC50 = 549.54 nM 6.26
CHEMBL4068969 — EC50 = 550.0 nM 6.26
CHEMBL4084094 — EC50 = 645.65 nM 6.19
CHEMBL4084094 — EC50 = 650.0 nM 6.19
CHEMBL4102082 — EC50 = 794.33 nM 6.10
CHEMBL4102082 — EC50 = 800.0 nM 6.10
CHEMBL4089962 — EC50 = 900.0 nM 6.05
CHEMBL4089962 — EC50 = 912.01 nM 6.04
CHEMBL4081667 — EC50 = 1200.0 nM 5.92
CHEMBL4061305 — EC50 = 1200.0 nM 5.92
CHEMBL4061305 — EC50 = 1230.27 nM 5.91
CHEMBL4081667 — EC50 = 1230.27 nM 5.91