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Compound Detail

CHEMBL5398686

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[2H]C([2H])([2H])N(Cc1ccccc1)c1ncnc2[nH]c(-c3ccc(CO)cc3)cc12

Basic Information

ChEMBL ID CHEMBL5398686
Phase Preclinical
Structure Type MOL
InChI Key KVBFMJDTLAIVSN-FIBGUPNXSA-N
Parent Compound CHEMBL5431583
Active Moiety CHEMBL5431583
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

344.4
MW (Da)
3.75
ALogP
4
HBA
2
HBD
65.0
PSA (Ų)
0.58
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20N4O
MW 347.44
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -0.73

Activity Summary

IC50 1 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 7.77 7.77 17.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 16.0 mL.min-1.g-1 Homo sapiens
CL 79.0 mL.min-1.g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 17.0 nM 7.77 Inhibition of EGFR (unknown origin) 37191268

Literature References

PubMed DOI Target Context # Activities
37191268 10.1021/acs.jmedchem.3c00428 ADMET 6
37191268 10.1021/acs.jmedchem.3c00428 No relevant target 1
37191268 10.1021/acs.jmedchem.3c00428 Macrophage colony-stimulating factor 1 receptor 1
37191268 10.1021/acs.jmedchem.3c00428 Epidermal growth factor receptor 1

Data from ChEMBL 36 via Core Engine