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Assay Detail

CHEMBL4040575

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Binding
Inhibition of glycosylated human ATX using LPC 16:0 as substrate after 30 mins by luminescence assay
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Autotaxin (CHEMBL3691) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.
Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B.
J Med Chem (2017) 60 : 7371 -7392
PubMed 28731719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.03 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061747 — — 1 7.57
CHEMBL4100092 — — 1 7.07
CHEMBL4069323 — — 1 6.90
CHEMBL4095636 — — 1 6.86
CHEMBL4073251 — — 1 6.64
CHEMBL4063869 — — 1 6.61
CHEMBL4064663 — — 1 6.58
CHEMBL4066101 — — 1 6.55
CHEMBL4081493 — — 1 6.45
CHEMBL4087476 — — 1 6.32
CHEMBL4083879 — — 1 6.31
CHEMBL4104285 — — 1 6.27
CHEMBL4099513 — — 1 6.15
CHEMBL4084600 — — 1 6.11
CHEMBL4080051 — — 1 6.09
CHEMBL4082953 — — 1 6.00
CHEMBL4062291 — — 1 5.92
CHEMBL4096556 — — 1 5.92
CHEMBL4066613 — — 1 5.85
CHEMBL4087120 — — 1 5.82
CHEMBL4092339 — — 1 5.79
CHEMBL4070910 — — 1 5.79
CHEMBL4061071 — — 1 5.77
CHEMBL4074310 — — 1 5.77
CHEMBL4099392 — — 1 5.72
CHEMBL4101875 — — 1 5.72
CHEMBL4098466 — — 1 5.69
CHEMBL4075235 — — 1 5.64
CHEMBL4091774 — — 1 5.63
CHEMBL4102549 — — 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061747 — IC50 = 27.0 nM 7.57
CHEMBL4100092 — IC50 = 86.0 nM 7.07
CHEMBL4069323 — IC50 = 126.0 nM 6.90
CHEMBL4095636 — IC50 = 138.0 nM 6.86
CHEMBL4073251 — IC50 = 231.0 nM 6.64
CHEMBL4063869 — IC50 = 246.0 nM 6.61
CHEMBL4064663 — IC50 = 261.0 nM 6.58
CHEMBL4066101 — IC50 = 280.0 nM 6.55
CHEMBL4081493 — IC50 = 357.0 nM 6.45
CHEMBL4087476 — IC50 = 480.0 nM 6.32
CHEMBL4083879 — IC50 = 493.0 nM 6.31
CHEMBL4104285 — IC50 = 533.0 nM 6.27
CHEMBL4099513 — IC50 = 710.0 nM 6.15
CHEMBL4084600 — IC50 = 771.0 nM 6.11
CHEMBL4080051 — IC50 = 804.0 nM 6.09
CHEMBL4082953 — IC50 = 1001.0 nM 6.00
CHEMBL4062291 — IC50 = 1210.0 nM 5.92
CHEMBL4096556 — IC50 = 1212.0 nM 5.92
CHEMBL4066613 — IC50 = 1410.0 nM 5.85
CHEMBL4087120 — IC50 = 1521.0 nM 5.82
CHEMBL4092339 — IC50 = 1614.0 nM 5.79
CHEMBL4070910 — IC50 = 1624.0 nM 5.79
CHEMBL4061071 — IC50 = 1684.0 nM 5.77
CHEMBL4074310 — IC50 = 1708.0 nM 5.77
CHEMBL4099392 — IC50 = 1899.0 nM 5.72
CHEMBL4101875 — IC50 = 1904.0 nM 5.72
CHEMBL4098466 — IC50 = 2021.0 nM 5.69
CHEMBL4075235 — IC50 = 2266.0 nM 5.64
CHEMBL4091774 — IC50 = 2359.0 nM 5.63
CHEMBL4102549 — IC50 = 2372.0 nM 5.62
CHEMBL4080946 — IC50 = 4246.0 nM 5.37
CHEMBL4073638 — IC50 = 6555.0 nM 5.18
CHEMBL4084005 — IC50 = 6800.0 nM 5.17
CHEMBL4072466 — IC50 = 7609.0 nM 5.12
CHEMBL4065695 — IC50 = 9163.0 nM 5.04
CHEMBL4094811 — IC50 > 4100.0 nM -
CHEMBL4100462 — IC50 > 10000.0 nM -
CHEMBL4084750 — IC50 > 10000.0 nM -
CHEMBL4091653 — IC50 > 10000.0 nM -
CHEMBL4087931 — IC50 > 10000.0 nM -