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Compound Detail

CHEMBL3735952

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COC1CCN(c2nccc(Nc3cc4[nH]cnc4cn3)n2)CC1

Basic Information

ChEMBL ID CHEMBL3735952
Phase Preclinical
Structure Type MOL
InChI Key VOVOJNOXHDWRNB-UHFFFAOYSA-N
2
Targets
4
Activities
3
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

325.4
MW (Da)
2.11
ALogP
7
HBA
2
HBD
91.8
PSA (Ų)
0.76
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H19N7O
MW 325.38
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.32

Activity Summary

Ki 2 meas. best 6.48
EC50 1 meas. best 5.16
IC50 1 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
Ki 6.48 6.2 329.0 2
Epidermal growth factor receptor
CHEMBL203
IC50 6.06 6.06 880.0 1
NCI-H1975
CHEMBL614348
EC50 5.16 5.16 7000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26455919 10.1021/acs.jmedchem.5b01412 Epidermal growth factor receptor 3
26455919 10.1021/acs.jmedchem.5b01412 No relevant target 1
26455919 10.1021/acs.jmedchem.5b01412 NCI-H1975 1

Data from ChEMBL 36 via Core Engine