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Assay Detail

CHEMBL5538868

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

Binding
Inhibition of human ATX in using LPC as substrate by fluorescence based microplate reader assay
24
Total Activities
24
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

Design, synthesis and evaluation of novel UDCA-aminopyrimidine hybrids as ATX inhibitors for the treatment of hepatic and pulmonary fibrosis.
Hu Y, Li L, Tian Y, Xiao Y, Tang J, Zeng S, Zou Z, Shang H.
Eur J Med Chem (2024) 264 : 116029 -116029
PubMed 38091892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.08 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566552 1 8.12
CHEMBL5575865 1 8.12
CHEMBL5591143 1 7.81
CHEMBL5575423 1 7.81
CHEMBL5595881 1 7.56
CHEMBL5562884 1 7.45
CHEMBL5574060 1 7.40
CHEMBL5569627 1 7.38
CHEMBL5568776 1 7.36
CHEMBL5567280 1 7.33
CHEMBL5567151 1 7.24
CHEMBL3828074 ZIRITAXESTAT 3.0 1 7.13
CHEMBL5569443 1 7.04
CHEMBL5569991 1 7.03
CHEMBL5564559 1 6.99
CHEMBL5572432 1 6.87
CHEMBL5574522 1 6.78
CHEMBL5595894 1 6.78
CHEMBL5572676 1 6.78
CHEMBL5594899 1 6.62
CHEMBL5573906 1 6.47
CHEMBL5571100 1 6.47
CHEMBL5565831 1 6.36
CHEMBL1551 URSODIOL 4.0 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566552 IC50 = 7.51 nM 8.12
CHEMBL5575865 IC50 = 7.62 nM 8.12
CHEMBL5591143 IC50 = 15.39 nM 7.81
CHEMBL5575423 IC50 = 15.57 nM 7.81
CHEMBL5595881 IC50 = 27.72 nM 7.56
CHEMBL5562884 IC50 = 35.61 nM 7.45
CHEMBL5574060 IC50 = 40.19 nM 7.40
CHEMBL5569627 IC50 = 41.42 nM 7.38
CHEMBL5568776 IC50 = 43.93 nM 7.36
CHEMBL5567280 IC50 = 46.29 nM 7.33
CHEMBL5567151 IC50 = 57.83 nM 7.24
CHEMBL3828074 ZIRITAXESTAT IC50 = 73.4 nM 7.13
CHEMBL5569443 IC50 = 91.72 nM 7.04
CHEMBL5569991 IC50 = 92.51 nM 7.03
CHEMBL5564559 IC50 = 102.42 nM 6.99
CHEMBL5572432 IC50 = 136.29 nM 6.87
CHEMBL5574522 IC50 = 165.11 nM 6.78
CHEMBL5595894 IC50 = 168.07 nM 6.78
CHEMBL5572676 IC50 = 164.75 nM 6.78
CHEMBL5594899 IC50 = 242.87 nM 6.62
CHEMBL5573906 IC50 = 335.34 nM 6.47
CHEMBL5571100 IC50 = 341.58 nM 6.47
CHEMBL5565831 IC50 = 438.35 nM 6.36
CHEMBL1551 URSODIOL IC50 = 9260.0 nM 5.03