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Compound Detail

CHEMBL3979972

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COc1cc(OC)cc(N(CC#Cc2ccncc2C#N)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3979972
Phase Preclinical
Structure Type MOL
InChI Key AGBXUKHUCRHKSZ-UHFFFAOYSA-N
6
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

501.6
MW (Da)
4.50
ALogP
9
HBA
0
HBD
102.0
PSA (Ų)
0.31
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H23N7O2
MW 501.55
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.30

Activity Summary

IC50 13 meas. best 8.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.11 6.7967 7.8 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.07 8.07 8.5 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 7.86 6.6667 13.8 3
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.52 6.39 30.2 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.2 7.2 63.1 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.12 6.015 758.6 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 7.762 nM 8.11 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 8.511 nM 8.07 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 13.8 nM 7.86 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 30.2 nM 7.52 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 4 IC50 = 63.1 nM 7.2 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 354.81 nM 6.45 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 478.63 nM 6.32 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 758.58 nM 6.12 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 1 IC50 = 1096.48 nM 5.96 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 1230.27 nM 5.91 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 1445.44 nM 5.84 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Vascular endothelial growth factor receptor 2 IC50 = 1548.82 nM 5.81 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Fibroblast growth factor receptor 3 IC50 = 2041.74 nM 5.69 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine