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Compound Detail

CHEMBL139229

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CN(C)CCNC(=O)c1cc(NC(=O)CCC(=O)Nc2cc(CO)cc(Nc3c4ccccc4nc4ccccc34)c2)cn1C

Basic Information

ChEMBL ID CHEMBL139229
Phase Preclinical
Structure Type MOL
InChI Key VGJBTLYKVSWBCN-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

607.7
MW (Da)
4.61
ALogP
8
HBA
5
HBD
140.6
PSA (Ų)
0.13
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H37N7O4
MW 607.72
Aromatic Rings 5
Heavy Atoms 45
NP-Likeness -0.92

Activity Summary

IC50 6 meas. best 6.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HONE1 cell line
CHEMBL614830
IC50 6.07 6.07 850.0 1
HT-29
CHEMBL384
IC50 5.77 5.77 1700.0 1
HepG2
CHEMBL395
IC50 5.38 5.38 4200.0 1
TSGH
CHEMBL615018
IC50 5.34 5.34 4600.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.16 5.125 7000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12238927 10.1021/jm0200714 NON-PROTEIN TARGET 2
12238927 10.1021/jm0200714 HT-29 1
12238927 10.1021/jm0200714 HONE1 cell line 1
12238927 10.1021/jm0200714 TSGH 1
12238927 10.1021/jm0200714 HepG2 1
12238927 10.1021/jm0200714 MX1 1
12238927 10.1021/jm0200714 CCRF-CEM 1
12238927 10.1021/jm0200714 Nucleic Acid 1

Data from ChEMBL 36 via Core Engine