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Compound Detail

CHEMBL123756

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C#CCN(Cc1cc2c(=O)n(C)c(CN3CCN(C)CC3)nc2cc1Cl)c1ccc(C(=O)NCc2cccnc2)cc1

Basic Information

ChEMBL ID CHEMBL123756
Phase Preclinical
Structure Type MOL
InChI Key LWTCFUSGPRGUBX-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

584.1
MW (Da)
3.30
ALogP
8
HBA
1
HBD
86.6
PSA (Ų)
0.30
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H34ClN7O2
MW 584.12
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.79

Activity Summary

IC50 5 meas. best 9.51
EC50 1 meas. best 9.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinamide phosphoribosyltransferase
CHEMBL1744525
IC50 9.51 9.51 0.3 1
WIL2
CHEMBL612809
IC50 9.49 9.4 0.3 2
WIL2
CHEMBL612809
EC50 9.31 9.31 0.5 1
Proteasome
CHEMBL612443
IC50 5.52 5.52 3000.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 4.89 4.89 13000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12166942 10.1021/jm011081s WIL2 2
12166942 10.1021/jm011081s No relevant target 2
21080724 10.1021/jm101145b Nicotinamide phosphoribosyltransferase 2
12166942 10.1021/jm011081s NON-PROTEIN TARGET 1
12166942 10.1021/jm011081s Thymidylate synthase 1
12166942 10.1021/jm011081s Proteasome 1
21080724 10.1021/jm101145b WIL2 1
21080724 10.1021/jm101145b HCT-116 1

Data from ChEMBL 36 via Core Engine