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Compound Detail

CHEMBL2385134

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CCN(Cc1cccnc1)C(=O)CN(c1ccc(O[11CH3])nc1)S(=O)(=O)c1ccccc1C

Basic Information

ChEMBL ID CHEMBL2385134
Phase Preclinical
Structure Type MOL
InChI Key KJPHTXTWFHVJIG-KTXUZGJCSA-N
Parent Compound CHEMBL2385132
Active Moiety CHEMBL2385132
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

454.6
MW (Da)
3.04
ALogP
6
HBA
0
HBD
92.7
PSA (Ų)
0.49
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26N4O4S
MW 453.55
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -2.18

Activity Summary

Ki 2 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin receptor type 2
CHEMBL4792
Ki 8.96 8.96 1.1 1
Orexin/Hypocretin receptor type 1
CHEMBL5113
Ki 6.05 6.05 900.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.1133 - Papio anubis

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23601709 10.1016/j.bmcl.2013.03.079 ADMET 2
23601709 10.1016/j.bmcl.2013.03.079 Brain 2
23601709 10.1016/j.bmcl.2013.03.079 Kidney 1
23601709 10.1016/j.bmcl.2013.03.079 Liver 1
23601709 10.1016/j.bmcl.2013.03.079 No relevant target 1
23891187 10.1016/j.bmcl.2013.06.057 Orexin receptor type 2 1
23891187 10.1016/j.bmcl.2013.06.057 Orexin/Hypocretin receptor type 1 1

Data from ChEMBL 36 via Core Engine