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Compound Detail

CHEMBL3701241

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C=CC(=O)N1CC(n2nc(C#Cc3cc(OC)cc(OC)c3)c3c(N)ncnc32)C1

Basic Information

ChEMBL ID CHEMBL3701241
Phase Preclinical
Structure Type MOL
InChI Key GYXODBZTJVUDOH-UHFFFAOYSA-N
6
Targets
16
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

404.4
MW (Da)
1.39
ALogP
8
HBA
1
HBD
108.4
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20N6O3
MW 404.43
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.63

Activity Summary

IC50 16 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 10.0 9.68 0.1 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.96 8.932 1.1 5
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.92 8.6333 1.2 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.77 8.4633 1.7 3
SNU-16
CHEMBL613529
IC50 8.13 8.13 7.4 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.52 5.52 3029.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 28.31 ng.hr.mL-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 0.1 nM 10.0 Measurement of Inhibitory Effect on FGFR3 Kinase Activity: The inhibitory effect... -
Fibroblast growth factor receptor 3 IC50 = 0.3 nM 9.52 Inhibition Assay: Purified recombinant human FGFR3 protein was purchased from Ca... -
Fibroblast growth factor receptor 3 IC50 = 0.3 nM 9.52 Measurement of Inhibitory Effect on FGFR3 Kinase Activity: The inhibitory effect... -
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 Inhibition Assay: When setting conditions for the measurement of the inhibitory ... -
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 FGFR2 Kinase Activity: When setting conditions for the measurement of the inhibi... -
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 Measurement of Inhibitory Effect on FGFR2 Kinase Activity: When setting conditio... -
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 Measurement of Inhibitory Effect on FGFR2 Kinase Activity: When setting conditio... -
Fibroblast growth factor receptor 1 IC50 = 1.2 nM 8.92 Measurement of Inhibitory Effect on FGFR1 Kinase Activity: When setting conditio... -
Fibroblast growth factor receptor 2 IC50 = 1.5 nM 8.82 Inhibition of human recombinant cytoplasmic domain FGFR2 (8 to 134 residues) inc... 37077386
Fibroblast growth factor receptor 4 IC50 = 1.7 nM 8.77 Measurement of Inhibitory Effect on FGFR4 Kinase Activity: The inhibitory effect... -
Fibroblast growth factor receptor 1 IC50 = 3.2 nM 8.49 Inhibition Assay: Purified recombinant human FGFR4 protein was purchased from Ca... -
Fibroblast growth factor receptor 1 IC50 = 3.2 nM 8.49 Measurement of Inhibitory Effect on FGFR1 Kinase Activity: When setting conditio... -
Fibroblast growth factor receptor 4 IC50 = 4.9 nM 8.31 Inhibition Assay: Purified recombinant human FGFR4 protein was purchased from Ca... -
Fibroblast growth factor receptor 4 IC50 = 4.9 nM 8.31 Measurement of Inhibitory Effect on FGFR4 Kinase Activity: The inhibitory effect... -
SNU-16 IC50 = 7.4 nM 8.13 Cytotoxicity against human SNU-16 cells assessed as inhibition of cell growth me... 37077386
Vascular endothelial growth factor receptor 2 IC50 = 3029.0 nM 5.52 Inhibition of N-terminal GST tagged recombinant human VEGFR2 (aa805 to 1356 resi... 37077386

Literature References

PubMed DOI Target Context # Activities
37077386 10.1021/acsmedchemlett.3c00006 ADMET 3
37077386 10.1021/acsmedchemlett.3c00006 Fibroblast growth factor receptor 2 1
37077386 10.1021/acsmedchemlett.3c00006 Vascular endothelial growth factor receptor 2 1
37077386 10.1021/acsmedchemlett.3c00006 SNU-16 1
37077386 10.1021/acsmedchemlett.3c00006 SNU1 1
37077386 10.1021/acsmedchemlett.3c00006 No relevant target 1

Data from ChEMBL 36 via Core Engine