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Compound Detail

CHEMBL4552354

BI 3017
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Cc1nccc(COC(=O)N2C[C@@H]3[C@@H](CNC(=O)c4ccc5[nH]nnc5c4)[C@@H]3C2)n1

Basic Information

ChEMBL ID CHEMBL4552354
Name BI 3017
Phase Preclinical
Structure Type MOL
InChI Key ZDITZGRCUFFQRS-PHZGNYQRSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

407.4
MW (Da)
1.30
ALogP
7
HBA
2
HBD
126.0
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21N7O3
MW 407.43
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.41

Activity Summary

IC50 2 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Autotaxin
CHEMBL3691
IC50 5.05 5.05 8900.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Autotaxin IC50 = 8900.0 nM 5.05 Biochemical assay: measurement of LPA (human) -
Autotaxin IC50 = 8900.0 nM 5.05 Affinity Biochemical interaction: (Biochemical assay (LPA measurement)) EUB00010... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507275 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL4507275 Epidermal growth factor receptor 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507275 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4507275 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL5058564 U2OS 9
- 10.6019/CHEMBL4507275 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507275 Unchecked 8
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.6019/CHEMBL5058564 Fibroblast 6
- 10.6019/CHEMBL5303304 Fibroblast 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507275 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL5303304 U2OS 4
- 10.6019/CHEMBL5303304 HEK-293T 4
- 10.6019/CHEMBL5058564 HEK-293T 3
- 10.6019/CHEMBL4507275 ALK tyrosine kinase receptor 3
- 10.6019/CHEMBL4507275 Hepatocyte growth factor receptor 3
- 10.6019/CHEMBL4507275 Ribosomal protein S6 kinase alpha-3 2

Data from ChEMBL 36 via Core Engine