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Compound Detail

CHEMBL262321

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Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)[C@@H](C)N)c1

Basic Information

ChEMBL ID CHEMBL262321
Phase Preclinical
Structure Type MOL
InChI Key CLCIJGHLOGXLMK-KBKXWFDOSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

616.6
MW (Da)
4.73
ALogP
5
HBA
2
HBD
99.0
PSA (Ų)
0.40
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 C32H43Cl2N5O3
MW 616.63
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness -1.02

Activity Summary

IC50 1 meas. best 5.54
Ki 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
Ki 9.15 9.15 0.7 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.54 5.54 2900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocortin receptor 4 Ki = 0.71 nM 9.15 Binding affinity at human MC4R 17822895
Cytochrome P450 3A4 IC50 = 2900.0 nM 5.54 Inhibition of microsomal CYP3A4 17822895

Literature References

PubMed DOI Target Context # Activities
17822895 10.1016/j.bmcl.2007.07.097 Melanocortin receptor 4 1
17822895 10.1016/j.bmcl.2007.07.097 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine