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Compound Detail

CHEMBL4847687

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COc1cc(OC)c(F)c(N2Cc3cnc4[nH]c(CN5CCOCC5)cc4c3N(C)C2=O)c1F

Basic Information

ChEMBL ID CHEMBL4847687
Phase Preclinical
Structure Type MOL
InChI Key XSNHNDWDZPRWCO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
4
Publications
0
Known Names

Molecular Properties

473.5
MW (Da)
3.27
ALogP
6
HBA
1
HBD
83.2
PSA (Ų)
0.61
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25F2N5O4
MW 473.48
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.76

Activity Summary

IC50 1 meas. best 7.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.54 7.54 29.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3879.22 ng.hr.mL-1 Rattus norvegicus
AUC 5587.06 ng.hr.mL-1 Macaca fascicularis
CL 31.0 % Rattus norvegicus
CL 8.0 % Macaca fascicularis
F 100.0 % Rattus norvegicus
F 53.0 % Macaca fascicularis
T1/2 1.4 hr Rattus norvegicus
T1/2 7.9 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 29.0 nM 7.54 Inhibition of phosphorylated FGFR2alpha in human KATO III stomach cancer cell li... 34269576

Literature References

PubMed DOI Target Context # Activities
34269576 10.1021/acs.jmedchem.1c00713 ADMET 10
34269576 10.1021/acs.jmedchem.1c00713 Unchecked 1
34269576 10.1021/acs.jmedchem.1c00713 No relevant target 1
34269576 10.1021/acs.jmedchem.1c00713 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine