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Compound Detail

CHEMBL4077485

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CN1CCC(C(=O)N2CCC(c3ccc(NC(=O)N4Cc5ccc(F)cc5C4)cc3)CC2)CC1

Basic Information

ChEMBL ID CHEMBL4077485
Phase Preclinical
Structure Type MOL
InChI Key AMJUQLCPNJLRGT-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

464.6
MW (Da)
4.42
ALogP
3
HBA
1
HBD
55.9
PSA (Ų)
0.73
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33FN4O2
MW 464.59
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.56

Activity Summary

IC50 1 meas. best 8.25
Ki 1 meas. best 8.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PC-3
CHEMBL390
IC50 8.25 8.25 5.6 1
Nicotinamide phosphoribosyltransferase
CHEMBL1744525
Ki 8.03 8.03 9.4 1

Pharmacokinetic Data

Parameter Value Units Species
CL 266.67 mL.min-1.kg-1 Mus musculus
CL 41.67 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28610984 10.1016/j.bmcl.2017.06.018 Liver 2
28610984 10.1016/j.bmcl.2017.06.018 Nicotinamide phosphoribosyltransferase 1
28610984 10.1016/j.bmcl.2017.06.018 PC-3 1

Data from ChEMBL 36 via Core Engine