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

CHEMBL4876826

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
CCN1CCN(Cc2cc3c4c(cnc3[nH]2)CN(c2c(F)c(OC)cc(OC)c2F)C(=O)N4C)CC1

Basic Information

ChEMBL ID CHEMBL4876826
Phase Preclinical
Structure Type MOL
InChI Key SRZAANLPOLQXJY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
4
Publications
0
Known Names

Molecular Properties

500.6
MW (Da)
3.57
ALogP
6
HBA
1
HBD
77.2
PSA (Ų)
0.56
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30F2N6O3
MW 500.55
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.71

Activity Summary

IC50 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.62 7.62 24.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 583.14 ng.hr.mL-1 Rattus norvegicus
AUC 2939.73 ng.hr.mL-1 Macaca fascicularis
CL 8.0 % Macaca fascicularis
CL 51.0 % Rattus norvegicus
F 49.0 % Rattus norvegicus
F 26.0 % Macaca fascicularis
T1/2 11.9 hr Rattus norvegicus
T1/2 12.0 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 24.0 nM 7.62 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 Cytochrome P450 3A4 2
34269576 10.1021/acs.jmedchem.1c00713 Unchecked 1
34269576 10.1021/acs.jmedchem.1c00713 No relevant target 1

Data from ChEMBL 36 via Core Engine