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Compound Detail

CHEMBL16458

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CCCC1=C(C(=O)OCc2ccc(C(=O)NCCN3CCCCC3)cc2)C(c2cccc(C)c2)NC(=O)N1

Basic Information

ChEMBL ID CHEMBL16458
Phase Preclinical
Structure Type MOL
InChI Key ZKQFZGPVBKPMOV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
2
Publications
0
Known Names

Molecular Properties

518.7
MW (Da)
4.36
ALogP
5
HBA
3
HBD
99.8
PSA (Ų)
0.41
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H38N4O4
MW 518.66
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.26

Activity Summary

EC50 1 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HEK293
CHEMBL614818
EC50 5.89 5.89 1300.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 65.0 % Rattus norvegicus
F 65.0 % Rattus norvegicus
F 13.0 % Rattus norvegicus
F 13.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HEK293 EC50 = 1300.0 nM 5.89 In vitro cAMP accumulation in HEK 293 cells. 14980655

Literature References

PubMed DOI Target Context # Activities
14980655 10.1016/j.bmcl.2003.12.071 Rattus norvegicus 4
14980655 10.1016/j.bmcl.2003.12.071 HEK293 2

Data from ChEMBL 36 via Core Engine