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Compound Detail

CHEMBL3647539

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CCn1cnc2c(-c3ccc(F)c(-c4ccc(S(=O)(=O)C5CC5)cc4OC)c3)cnnc21

Basic Information

ChEMBL ID CHEMBL3647539
Phase Preclinical
Structure Type MOL
InChI Key LYBURRCIXUSBMB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

452.5
MW (Da)
4.26
ALogP
7
HBA
0
HBD
87.0
PSA (Ų)
0.43
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21FN4O3S
MW 452.51
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.29

Activity Summary

Ki 2 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL4956
Ki 8.01 8.01 9.7 1
Unchecked
CHEMBL612545
Ki 7.9 7.9 12.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 12.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30964988 10.1021/acs.jmedchem.9b00322 Unchecked 2
30964988 10.1021/acs.jmedchem.9b00322 ADMET 2
30964988 10.1021/acs.jmedchem.9b00322 GABA-A receptor; alpha-1/beta-3/gamma-2 1
30964988 10.1021/acs.jmedchem.9b00322 No relevant target 1

Data from ChEMBL 36 via Core Engine