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Compound Detail

CHEMBL2023489

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COc1ccc2c(Oc3ccc(CC(=O)Nc4cn(C)nc4C)c(OC)c3)ccnc2c1

Basic Information

ChEMBL ID CHEMBL2023489
Phase Preclinical
Structure Type MOL
InChI Key YYPVGQBXTJNGFW-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
5
PK Parameters
14
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
4.27
ALogP
7
HBA
1
HBD
87.5
PSA (Ų)
0.47
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24N4O4
MW 432.48
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.14

Activity Summary

IC50 5 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Platelet-derived growth factor receptor alpha
CHEMBL2007
IC50 8.52 8.52 3.0 1
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 8.4 8.4 4.0 1
Hepatocyte growth factor receptor
CHEMBL3717
IC50 8.4 8.4 4.0 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 6.7 6.7 200.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 4.96 4.96 10990.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.4 mL.min-1.kg-1 Canis lupus familiaris
CL 23.44 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL 24.55 mL.min-1.g-1 Homo sapiens
T1/2 3.7 hr Rattus norvegicus
T1/2 8.6 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22497760 10.1016/j.bmcl.2012.03.074 Rattus norvegicus 10
22497760 10.1016/j.bmcl.2012.03.074 C6 3
22497760 10.1016/j.bmcl.2012.03.074 Canis familiaris 3
- 10.6019/CHEMBL3301361 ADMET 3
30204441 10.1021/acs.jmedchem.8b00938 Mast/stem cell growth factor receptor Kit 3
- 10.6019/CHEMBL3301361 No relevant target 2
22497760 10.1016/j.bmcl.2012.03.074 Platelet-derived growth factor receptor beta 1
22497760 10.1016/j.bmcl.2012.03.074 Macrophage colony-stimulating factor 1 receptor 1
22497760 10.1016/j.bmcl.2012.03.074 Vascular endothelial growth factor receptor 2 1
22497760 10.1016/j.bmcl.2012.03.074 Platelet-derived growth factor receptor alpha 1
22497760 10.1016/j.bmcl.2012.03.074 Receptor-type tyrosine-protein kinase FLT3 1
30204441 10.1021/acs.jmedchem.8b00938 BaF3 1
30204441 10.1021/acs.jmedchem.8b00938 Vascular endothelial growth factor receptor 2 1
38492541 10.1016/j.bmc.2024.117681 Hepatocyte growth factor receptor 1

Data from ChEMBL 36 via Core Engine