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Compound Detail

CHEMBL5613363

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CC(C)(C)c1ccc(NC(=O)NCCCN(CCCN2CCOCC2)CC2(O)CCN(c3ncnc4[nH]cnc34)C2)cc1

Basic Information

ChEMBL ID CHEMBL5613363
Phase Preclinical
Structure Type MOL
InChI Key QRGXBNWFMKGFND-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

593.8
MW (Da)
2.83
ALogP
9
HBA
4
HBD
134.8
PSA (Ų)
0.23
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H47N9O3
MW 593.78
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -1.39

Activity Summary

IC50 1 meas. best 4.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H460
CHEMBL396
IC50 4.14 4.14 73070.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NCI-H460 IC50 = 73070.0 nM 4.14 Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mu... 39255403

Literature References

PubMed DOI Target Context # Activities
39255403 10.1021/acs.jmedchem.4c01096 NCI-H460 2

Data from ChEMBL 36 via Core Engine