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Compound Detail

CHEMBL4856966

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COc1cc(OC)c(F)c(N2Cc3cnc4c(c3N(C)C2=O)CC(=O)N4)c1F

Basic Information

ChEMBL ID CHEMBL4856966
Phase Preclinical
Structure Type MOL
InChI Key YPQHVWLVVJREBV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
9
PK Parameters
3
Publications
0
Known Names

Molecular Properties

390.4
MW (Da)
2.45
ALogP
5
HBA
1
HBD
84.0
PSA (Ų)
0.87
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H16F2N4O4
MW 390.35
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.28

Activity Summary

IC50 1 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.46 7.46 35.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1366.23 ng.hr.mL-1 Rattus norvegicus
AUC 823.25 ng.hr.mL-1 Macaca fascicularis
CL 12.0 % Macaca fascicularis
CL 8.333 mL.min-1.kg-1 Homo sapiens
CL 34.0 % Rattus norvegicus
F 74.0 % Rattus norvegicus
F 24.0 % Macaca fascicularis
T1/2 1.3 hr Rattus norvegicus
T1/2 2.8 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 35.0 nM 7.46 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 12
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