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Compound Detail

CHEMBL3734934

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CC(C)n1c(CO)nc2cnc(Nc3ccnc(N4CC[C@H](O)[C@H](F)C4)n3)cc21

Basic Information

ChEMBL ID CHEMBL3734934
Phase Preclinical
Structure Type MOL
InChI Key BPMVYYLSRDJWNL-DOMZBBRYSA-N
1
Targets
2
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

401.4
MW (Da)
1.95
ALogP
9
HBA
3
HBD
112.2
PSA (Ų)
0.59
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H24FN7O2
MW 401.45
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.17

Activity Summary

IC50 1 meas. best 5.6
Ki 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
Ki 7.8 7.8 16.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.6 5.6 2530.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 151.0 mL.min-1.kg-1 Rattus norvegicus
CL 382.0 mL.min-1.kg-1 Rattus norvegicus

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 4
26455919 10.1021/acs.jmedchem.5b01412 Rattus norvegicus 2
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