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Compound Detail

CHEMBL4552180

BAY-588
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Cc1c(NC(=O)c2cc(C(N)=O)nc3cc(F)ccc23)c(C(F)(F)F)nn1Cc1ccc(C(C)(C)C)cc1

Basic Information

ChEMBL ID CHEMBL4552180
Name BAY-588
Phase Preclinical
Structure Type MOL
InChI Key DNGZBWVQLFNTRT-UHFFFAOYSA-N
3
Targets
9
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

527.5
MW (Da)
5.59
ALogP
5
HBA
2
HBD
102.9
PSA (Ų)
0.33
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25F4N5O2
MW 527.52
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.70

Activity Summary

IC50 9 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Solute carrier family 2, facilitated glucose transporter member 4
CHEMBL5874
IC50 6.3 6.3 500.0 3
Solute carrier family 2, facilitated glucose transporter member 1
CHEMBL2535
IC50 5.93 5.9233 1180.0 3
Solute carrier family 2, facilitated glucose transporter member 3
CHEMBL5215
IC50 5.26 5.26 5470.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Solute carrier family 2, facilitated glucose transporter member 4 IC50 = 500.0 nM 6.3 Cell-based assay with CellTiter-Glo readout for ATP production with SLC2A4 -
Solute carrier family 2, facilitated glucose transporter member 4 IC50 = 500.0 nM 6.3 Selectivity interaction (Glucose transporter panel (CellTiter-Glo® Luminescent C... -
Solute carrier family 2, facilitated glucose transporter member 4 IC50 = 500.0 nM 6.3 Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucos... 27552707
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 1180.0 nM 5.93 Inhibition of human GLUT1 expressed in human DLD-1 cells assessed as reduction i... 27552707
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 1200.0 nM 5.92 Cell-based assay with CellTiter-Glo readout for ATP production with SLC2A1 -
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 1200.0 nM 5.92 Affinity On-target Cellular interaction (CellTiter-Glo® Luminescent Cell Viabili... -
Solute carrier family 2, facilitated glucose transporter member 3 IC50 = 5500.0 nM 5.26 Cell-based assay with CellTiter-Glo readout for ATP production with SLC2A3 -
Solute carrier family 2, facilitated glucose transporter member 3 IC50 = 5500.0 nM 5.26 Selectivity interaction (Glucose transporter panel (CellTiter-Glo® Luminescent C... -
Solute carrier family 2, facilitated glucose transporter member 3 IC50 = 5470.0 nM 5.26 Inhibition of human GLUT3 expressed in human GLUT1-/- DLD-1 cells assessed as re... 27552707

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507267 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507267 Epidermal growth factor receptor 12
- 10.6019/CHEMBL4507267 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4689842 HEK-293T 10
- 10.6019/CHEMBL4507267 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4689842 Fibroblast 9
- 10.6019/CHEMBL4507267 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507267 Unchecked 8
- 10.6019/CHEMBL4689842 U2OS 6
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507267 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507267 Hepatocyte growth factor receptor 3
- 10.6019/CHEMBL4507267 ALK tyrosine kinase receptor 3
- 10.6019/CHEMBL4507267 Tyrosine-protein kinase JAK1 2
- 10.6019/CHEMBL4507267 Ribosomal protein S6 kinase alpha-5 2
- 10.6019/CHEMBL4507267 Ribosomal protein S6 kinase alpha-4 2
- 10.6019/CHEMBL4507267 Ribosomal protein S6 kinase alpha-1 2

Data from ChEMBL 36 via Core Engine