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Assay Detail

CHEMBL4143973

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

Binding
Inhibition of recombinant rat ATX using LPC 18:1 as substrate after 2 hrs by rapidfire/MS-based analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Autotaxin (CHEMBL3826870)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.
Kuttruff CA, Ferrara M, Bretschneider T, Hoerer S, Handschuh S, Nosse B, Romig H, Nicklin P, Roth GJ.
ACS Med Chem Lett (2017) 8 : 1252 -1257
PubMed 29259743 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.94 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4172309 1 8.89
CHEMBL4173049 1 8.82
CHEMBL4162641 1 8.77
CHEMBL4168498 1 8.72
CHEMBL4169550 1 8.64
CHEMBL4173341 1 8.64
CHEMBL4169912 1 8.51
CHEMBL4165749 BI 2545 1 8.47
CHEMBL4170966 1 8.32
CHEMBL4169136 1 8.26
CHEMBL4164935 1 8.00
CHEMBL4163050 1 7.86
CHEMBL4159308 1 7.31
CHEMBL4164658 1 7.17
CHEMBL4174042 1 7.08
CHEMBL4171105 1 5.82
CHEMBL4162674 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4172309 IC50 = 1.3 nM 8.89
CHEMBL4173049 IC50 = 1.5 nM 8.82
CHEMBL4162641 IC50 = 1.7 nM 8.77
CHEMBL4168498 IC50 = 1.9 nM 8.72
CHEMBL4169550 IC50 = 2.3 nM 8.64
CHEMBL4173341 IC50 = 2.3 nM 8.64
CHEMBL4169912 IC50 = 3.1 nM 8.51
CHEMBL4165749 BI 2545 IC50 = 3.4 nM 8.47
CHEMBL4170966 IC50 = 4.8 nM 8.32
CHEMBL4169136 IC50 = 5.5 nM 8.26
CHEMBL4164935 IC50 = 10.0 nM 8.00
CHEMBL4163050 IC50 = 13.9 nM 7.86
CHEMBL4159308 IC50 = 49.0 nM 7.31
CHEMBL4164658 IC50 = 66.9 nM 7.17
CHEMBL4174042 IC50 = 82.6 nM 7.08
CHEMBL4171105 IC50 = 1530.0 nM 5.82
CHEMBL4162674 IC50 = 1674.0 nM 5.78