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Assay Detail

CHEMBL5388522

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

Functional
Antagonist activity at human LPA1 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization pretreated for 15 mins followed by LPA stimulation by FLIPR analysis
62
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysophosphatidic acid receptor 1 (CHEMBL3819)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent, Selective, and Orally Bioavailable Tool Compound for Probing the Role of Lysophosphatidic Acid Type 2 Receptor Antagonists in Fibrotic Disorders.
Armani E, Rizzi A, Iotti N, Saccani F, Di Lascia MR, Tigli L, Pappani A, Marchini G, Murgo A, Capelli AM, Delcanale M, Puccini P, Villetti G, Civelli M, Beato C, Giuliani M, Mundi C, Murarolli F, Pagano M, Raveglia LF, Remelli R, Amari G.
J Med Chem (2023) 66 : 5622 -5656
PubMed 37017110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 4.83 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5413416 1 6.09
CHEMBL5401368 2 5.27
CHEMBL5418117 1 5.25
CHEMBL5398116 1 5.06
CHEMBL5439647 1 5.02
CHEMBL256470 1 5.01
CHEMBL5399781 2 5.00
CHEMBL5406143 1 4.99
CHEMBL5409858 1 4.98
CHEMBL5403072 1 4.98
CHEMBL5396575 1 4.98
CHEMBL5419697 1 4.91
CHEMBL5434862 2 4.90
CHEMBL5407919 1 4.89
CHEMBL5427680 1 4.82
CHEMBL5404276 1 4.82
CHEMBL5429482 1 4.81
CHEMBL5405375 1 4.77
CHEMBL5435934 1 4.75
CHEMBL5436208 1 4.74
CHEMBL5410659 1 4.74
CHEMBL5438524 1 4.72
CHEMBL5417982 1 4.72
CHEMBL5396746 1 4.72
CHEMBL5421405 1 4.69
CHEMBL5407268 1 4.69
CHEMBL5405856 1 4.67
CHEMBL5418255 1 4.66
CHEMBL5433347 1 4.66
CHEMBL5428223 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5413416 IC50 = 812.83 nM 6.09
CHEMBL5401368 IC50 = 5370.32 nM 5.27
CHEMBL5418117 IC50 = 5623.41 nM 5.25
CHEMBL5398116 IC50 = 8709.64 nM 5.06
CHEMBL5401368 IC50 = 9120.11 nM 5.04
CHEMBL5439647 IC50 = 9549.93 nM 5.02
CHEMBL256470 IC50 = 9772.37 nM 5.01
CHEMBL5399781 IC50 = 10000.0 nM 5.00
CHEMBL5406143 IC50 = 10232.93 nM 4.99
CHEMBL5409858 IC50 = 10471.29 nM 4.98
CHEMBL5403072 IC50 = 10471.29 nM 4.98
CHEMBL5396575 IC50 = 10471.29 nM 4.98
CHEMBL5399781 IC50 = 11748.98 nM 4.93
CHEMBL5419697 IC50 = 12302.69 nM 4.91
CHEMBL5434862 IC50 = 12589.25 nM 4.90
CHEMBL5407919 IC50 = 12882.5 nM 4.89
CHEMBL5404276 IC50 = 15135.61 nM 4.82
CHEMBL5427680 IC50 = 15135.61 nM 4.82
CHEMBL5429482 IC50 = 15488.17 nM 4.81
CHEMBL5405375 IC50 = 16982.44 nM 4.77
CHEMBL5435934 IC50 = 17782.79 nM 4.75
CHEMBL5436208 IC50 = 18197.01 nM 4.74
CHEMBL5410659 IC50 = 18197.01 nM 4.74
CHEMBL5396746 IC50 = 19054.61 nM 4.72
CHEMBL5438524 IC50 = 19054.61 nM 4.72
CHEMBL5417982 IC50 = 19054.61 nM 4.72
CHEMBL5421405 IC50 = 20417.38 nM 4.69
CHEMBL5407268 IC50 = 20417.38 nM 4.69
CHEMBL5405856 IC50 = 21379.62 nM 4.67
CHEMBL5418255 IC50 = 21877.62 nM 4.66
CHEMBL5433347 IC50 = 21877.62 nM 4.66
CHEMBL5428223 IC50 = 23988.33 nM 4.62
CHEMBL5429728 IC50 = 27542.29 nM 4.56
CHEMBL5408817 IC50 = 30902.95 nM 4.51
CHEMBL5440548 IC50 = 31622.78 nM 4.50
CHEMBL5411589 IC50 = 31622.78 nM 4.50
CHEMBL5396450 IC50 = 33113.11 nM 4.48
CHEMBL5411654 IC50 = 36307.81 nM 4.44
CHEMBL5434883 IC50 = 40738.03 nM 4.39
CHEMBL5399159 IC50 > 50118.72 nM -
CHEMBL5405450 IC50 > 50118.72 nM -
CHEMBL5427161 IC50 > 50118.72 nM -
CHEMBL5395244 IC50 > 50118.72 nM -
CHEMBL5424571 IC50 > 50118.72 nM -
CHEMBL5434096 IC50 > 50118.72 nM -
CHEMBL5418199 IC50 > 50118.72 nM -
CHEMBL5424251 IC50 > 5011.87 nM -
CHEMBL5424662 IC50 > 50118.72 nM -
CHEMBL5397550 IC50 > 501.19 nM -
CHEMBL5393777 IC50 > 50118.72 nM -