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Compound Detail

CHEMBL4778844

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COc1cc2nc(N3CCN(C(=O)c4ccc(NC(=O)COCC(=O)Nc5ccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)cc5)cc4)CC3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL4778844
Phase Preclinical
Structure Type MOL
InChI Key OJADKMIAMHTIRW-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

915.0
MW (Da)
3.29
ALogP
17
HBA
4
HBD
255.1
PSA (Ų)
0.12
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H50N12O9
MW 914.98
Aromatic Rings 6
Heavy Atoms 67
NP-Likeness -0.77

Activity Summary

IC50 2 meas. best 4.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
U-251
CHEMBL615022
IC50 4.52 4.52 30440.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
U-251 IC50 = 30440.0 nM 4.52 Antiproliferative activity against human U251 cells overexpressing EPHA2 assesse... 32828423

Literature References

PubMed DOI Target Context # Activities
32828423 10.1016/j.bmc.2020.115656 U-251 2
32828423 10.1016/j.bmc.2020.115656 Unchecked 1

Data from ChEMBL 36 via Core Engine