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Compound Detail

CHEMBL3622666

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O=C(/C=C/CNC1CC1)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1

Basic Information

ChEMBL ID CHEMBL3622666
Phase Preclinical
Structure Type MOL
InChI Key RVSQKIFMHKORJJ-IMLGJKEDSA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
6
Publications
0
Known Names

Molecular Properties

498.0
MW (Da)
4.58
ALogP
7
HBA
3
HBD
97.4
PSA (Ų)
0.37
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25ClFN5O3
MW 497.96
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.11

Activity Summary

IC50 1 meas. best 8.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 8.19 8.19 6.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 659.6 ng.hr.mL-1 Rattus norvegicus
AUC 662.4 ng.hr.mL-1 Rattus norvegicus
CL 25.67 mL.min-1.kg-1 Rattus norvegicus
F 83.47 % Rattus norvegicus
MRT 3.88 hr Rattus norvegicus
T1/2 3.15 hr Rattus norvegicus
Vd 3.82 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 6.5 nM 8.19 Inhibition of EGFR (unknown origin) by ELISA method 26310890

Literature References

PubMed DOI Target Context # Activities
26310890 10.1016/j.ejmech.2015.08.026 Mus musculus 11
26310890 10.1016/j.ejmech.2015.08.026 Rattus norvegicus 7
26310890 10.1016/j.ejmech.2015.08.026 NCI-H1975 2
26310890 10.1016/j.ejmech.2015.08.026 A-431 2
26310890 10.1016/j.ejmech.2015.08.026 Epidermal growth factor receptor 1
26310890 10.1016/j.ejmech.2015.08.026 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine