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Compound Detail

CHEMBL4575416

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CCn1cnc2c(-c3ccnc(Oc4cccc(S(=O)(=O)CC)c4)c3)cnnc21

Basic Information

ChEMBL ID CHEMBL4575416
Phase Preclinical
Structure Type MOL
InChI Key CWBDUNBBWXYMAI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

409.5
MW (Da)
3.49
ALogP
8
HBA
0
HBD
99.9
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19N5O3S
MW 409.47
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.78

Activity Summary

Ki 1 meas. best 5.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 5.94 5.94 1141.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 1141.9 nM 5.94 Displacement of [3H]Ro-15-1788 from human GABA alpha2/beta2/gamma2 receptor expr... 30964988

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