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Compound Detail

CHEMBL4464593

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CC(C)n1cnc2c(-c3ccc(F)c(Oc4ccc(C#N)cn4)c3)cnnc21

Basic Information

ChEMBL ID CHEMBL4464593
Phase Preclinical
Structure Type MOL
InChI Key ZZQLOXLBQDPKAG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

374.4
MW (Da)
4.27
ALogP
7
HBA
0
HBD
89.5
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15FN6O
MW 374.38
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.85

Activity Summary

Ki 1 meas. best 6.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 6.45 6.45 358.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 38.0 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 = 358.3 nM 6.45 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