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Compound Detail

CHEMBL4287868

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C#CCOc1ccc(C(=O)c2ccc(NC(=O)C(=O)NCCc3ccc(OC)cc3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL4287868
Phase Preclinical
Structure Type MOL
InChI Key KCFAFIPZMQARCW-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

456.5
MW (Da)
3.24
ALogP
5
HBA
2
HBD
93.7
PSA (Ų)
0.29
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 C27H24N2O5
MW 456.50
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.12

Activity Summary

EC50 4 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H2122
CHEMBL1075533
EC50 7.55 7.55 28.0 1
NCI-H1155
CHEMBL2366073
EC50 6.92 5.5967 120.0 3

Pharmacokinetic Data

Parameter Value Units Species
T1/2 48.0 hr Homo sapiens
T1/2 28.0 hr Homo sapiens
T1/2 2.1 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29869888 10.1021/acs.jmedchem.8b00052 NCI-H1155 4
29869888 10.1021/acs.jmedchem.8b00052 ADMET 3
29869888 10.1021/acs.jmedchem.8b00052 Cytochrome P450 4F11 1
29869888 10.1021/acs.jmedchem.8b00052 NCI-H2122 1

Data from ChEMBL 36 via Core Engine