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Compound Detail

CHEMBL4849808

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COc1cc(OC)c(F)c(N2Cc3cnc4[nH]ccc4c3N(C3CCN(C)CC3)C2=O)c1F

Basic Information

ChEMBL ID CHEMBL4849808
Phase Preclinical
Structure Type MOL
InChI Key QBOZLDNDPSGSFT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
3.90
ALogP
5
HBA
1
HBD
73.9
PSA (Ų)
0.64
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25F2N5O3
MW 457.48
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.54

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 365.98 ng.hr.mL-1 Rattus norvegicus
CL 13.33 mL.min-1.kg-1 Homo sapiens
CL 21.0 % Rattus norvegicus
F 12.0 % Rattus norvegicus
T1/2 9.2 hr Rattus norvegicus

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 7
34269576 10.1021/acs.jmedchem.1c00713 Unchecked 1

Data from ChEMBL 36 via Core Engine