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Compound Detail

CHEMBL4100583

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CC[C@@]1(O)CC[C@H]2[C@H](CC[C@@H]3[C@@H]2CC[C@]2(C)[C@@H](C(=O)Cn4cc(C#N)cn4)CC[C@@H]32)C1

Basic Information

ChEMBL ID CHEMBL4100583
Phase Preclinical
Structure Type MOL
InChI Key VCXHZQXVKCMJJU-HXKXIXNFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

423.6
MW (Da)
4.73
ALogP
5
HBA
1
HBD
78.9
PSA (Ų)
0.76
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H37N3O2
MW 423.60
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness 0.76

Activity Summary

IC50 1 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.44 7.44 36.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 36.0 nM 7.44 Displacement of [35S]TBPS from GABA-A receptor in Sprague-Dawley rat cerebral co... 28753313

Literature References

PubMed DOI Target Context # Activities
28753313 10.1021/acs.jmedchem.7b00846 GABA-A receptor; alpha-1/beta-2/gamma-2 2
28753313 10.1021/acs.jmedchem.7b00846 Unchecked 1
28753313 10.1021/acs.jmedchem.7b00846 Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta 1
28753313 10.1021/acs.jmedchem.7b00846 GABA-A receptor alpha-4/beta-3/delta 1

Data from ChEMBL 36 via Core Engine