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Compound Detail

CHEMBL4204566

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C=CC(=O)N[C@H]1CN(c2nc(Nc3cnn(C)c3)c3ncn(C(C)C)c3n2)C[C@@H]1F

Basic Information

ChEMBL ID CHEMBL4204566
Phase Preclinical
Structure Type MOL
InChI Key IRMHXRHXLFRZFM-KBPBESRZSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

413.5
MW (Da)
1.71
ALogP
9
HBA
2
HBD
105.8
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H24FN9O
MW 413.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.32

Activity Summary

IC50 1 meas. best 6.15
Ki 1 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
Ki 6.82 6.82 152.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 6.15 6.15 713.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28287730 10.1021/acs.jmedchem.6b01894 Epidermal growth factor receptor 4
28287730 10.1021/acs.jmedchem.6b01894 No relevant target 2

Data from ChEMBL 36 via Core Engine