Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL3907479

FGFR INHIBITOR DEBIO 1347
🧪 Phase II
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
🧪 Phase II
Cc1nc2ccc(-n3ncc(C(=O)c4cc5ccccc5[nH]4)c3N)cc2[nH]1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3907479
Name FGFR INHIBITOR DEBIO 1347
Phase Phase II
Structure Type MOL
InChI Key BEMNJULZEQTDJY-UHFFFAOYSA-N

Known Names

Fgfr inhibitor debio 1347
13
Targets
26
Activities
2
Assay Types
4
PK Parameters
20
Publications
1
Known Names
2
Indications
3
Mechanisms

Molecular Properties

356.4
MW (Da)
3.35
ALogP
5
HBA
3
HBD
105.4
PSA (Ų)
0.43
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Natural Product

Extended Properties

Molecular Formula C20H16N6O
MW 356.39
Aromatic Rings 5
Heavy Atoms 27
NP-Likeness -1.65

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Fibroblast growth factor receptor 2 inhibitor INHIBITOR Fibroblast growth factor receptor 2 ✓ ✓
Fibroblast growth factor receptor 3 inhibitor INHIBITOR Fibroblast growth factor receptor 3 ✓ ✓
Fibroblast growth factor receptor 1 inhibitor INHIBITOR Fibroblast growth factor receptor 1 ✓ ✓

Indications

Neoplasms Breast Neoplasms

Activity Summary

IC50 21 meas. best 8.3
Kd 5 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
 Kd 8.52 8.52 3.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
 IC50 8.3 8.0975 5.0 4
Ephrin type-B receptor 6
CHEMBL5836
 Kd 8.15 8.15 7.0 1
Fibroblast growth factor receptor 2
CHEMBL4142
 IC50 8.12 8.0 7.6 4
NON-PROTEIN TARGET
CHEMBL3879801
 IC50 7.77 6.5 17.0 2
MAP kinase-activated protein kinase 2
CHEMBL2208
 Kd 7.75 7.75 18.0 1
Fibroblast growth factor receptor 3
CHEMBL2742
 IC50 7.75 7.6825 18.0 4
Histone deacetylase 6
CHEMBL1865
 IC50 7.08 7.08 83.8 1
Fibroblast growth factor receptor 4
CHEMBL3973
 IC50 6.54 6.54 290.0 2
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
 Kd 6.11 6.11 783.0 1
Pyridoxal kinase
CHEMBL1075181
 Kd 5.68 5.68 2110.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
 IC50 5.68 5.68 2100.0 2
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
 IC50 5.23 5.23 5900.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
 IC50 5.16 5.16 6900.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 102000.0 ng.hr.mL-1 Rattus norvegicus
AUC 26000.0 ng.hr.mL-1 Homo sapiens
CL 13.0 mL.min-1.g-1 Homo sapiens
F 30.0 % Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 Kd = 3.0 nM 8.52 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Fibroblast growth factor receptor 1 IC50 = 5.0 nM 8.3 Inhibition Kinase Activity Assay: The FGFR1 inhibitory activities of compounds w... -
Ephrin type-B receptor 6 Kd = 7.0 nM 8.15 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Fibroblast growth factor receptor 2 IC50 = 7.6 nM 8.12 Inhibition of human FGFR2 by time-resolved fluorescence or time-resolved fluores... 27933954
Fibroblast growth factor receptor 2 IC50 = 7.6 nM 8.12 Inhibition of FGFR2 (unknown origin) 29259745
Fibroblast growth factor receptor 2 IC50 = 7.6 nM 8.12 Inhibition of FGFR2 (unknown origin) 27914362
Fibroblast growth factor receptor 1 IC50 = 9.3 nM 8.03 Inhibition of human FGFR1 by time-resolved fluorescence or time-resolved fluores... 27933954
Fibroblast growth factor receptor 1 IC50 = 9.3 nM 8.03 Inhibition of FGFR1 (unknown origin) 27914362
Fibroblast growth factor receptor 1 IC50 = 9.3 nM 8.03 Inhibition of FGFR1 (unknown origin) 29259745
NON-PROTEIN TARGET IC50 = 17.0 nM 7.77 Antiproliferative activity against human SNU16 cells incubated for 4 days by CCK... 27933954
Fibroblast growth factor receptor 3 IC50 = 18.0 nM 7.75 Inhibition Kinase Activity Assay: The FGFR3 inhibitory activities of compounds l... -
MAP kinase-activated protein kinase 2 Kd = 18.0 nM 7.75 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Fibroblast growth factor receptor 3 IC50 = 22.0 nM 7.66 Inhibition of human FGFR3 by time-resolved fluorescence or time-resolved fluores... 27933954
Fibroblast growth factor receptor 3 IC50 = 22.0 nM 7.66 Inhibition of FGFR3 (unknown origin) 27914362
Fibroblast growth factor receptor 3 IC50 = 22.0 nM 7.66 Inhibition of FGFR3 (unknown origin) 29259745
Fibroblast growth factor receptor 2 IC50 = 23.0 nM 7.64 Inhibition Kinase Activity Assay: The FGFR2 inhibitory activities of compounds l... -
Histone deacetylase 6 IC50 = 83.75 nM 7.08 Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 wi... -
Fibroblast growth factor receptor 4 IC50 = 290.0 nM 6.54 Inhibition of FGFR4 (unknown origin) 27914362
Fibroblast growth factor receptor 4 IC50 = 290.0 nM 6.54 Inhibition of human FGFR4 by time-resolved fluorescence or time-resolved fluores... 27933954
Proto-oncogene tyrosine-protein kinase receptor Ret Kd = 783.0 nM 6.11 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878

Literature References

PubMed DOI Target Context # Activities
27933954 10.1021/acs.jmedchem.6b01156 NON-PROTEIN TARGET 11
29191878 10.1126/science.aan4368 Unchecked 5
- 10.6019/CHEMBL4808148 Histone deacetylase 6 4
27933954 10.1021/acs.jmedchem.6b01156 ADMET 3
27933954 10.1021/acs.jmedchem.6b01156 Voltage-gated inwardly rectifying potassium channel KCNH2 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
27933954 10.1021/acs.jmedchem.6b01156 Molecular identity unknown 2
27933954 10.1021/acs.jmedchem.6b01156 Rattus norvegicus 2
27933954 10.1021/acs.jmedchem.6b01156 Fibroblast growth factor receptor 1 2
27933954 10.1021/acs.jmedchem.6b01156 Fibroblast growth factor receptor 2 2
27933954 10.1021/acs.jmedchem.6b01156 Fibroblast growth factor receptor 3 2
27933954 10.1021/acs.jmedchem.6b01156 No relevant target 1
27933954 10.1021/acs.jmedchem.6b01156 Unchecked 1
27933954 10.1021/acs.jmedchem.6b01156 Mus musculus 1
29191878 10.1126/science.aan4368 AP2-associated protein kinase 1 1
29191878 10.1126/science.aan4368 Tyrosine-protein kinase ABL1 1
29191878 10.1126/science.aan4368 Acyl-CoA dehydrogenase family member 10 1
29191878 10.1126/science.aan4368 Peroxisomal acyl-coenzyme A oxidase 3 1
35436119 10.1021/acs.jmedchem.1c01776 BaF3 1

Data from ChEMBL 36 via Core Engine