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Compound Detail

CHEMBL4537552

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C#Cc1ccc2c(c1)C(c1ccccc1F)=N[C@H](C)c1c(C(=O)N(C)C)ncn1-2

Basic Information

ChEMBL ID CHEMBL4537552
Phase Preclinical
Structure Type MOL
InChI Key LNPOWXXHIUMIKI-CQSZACIVSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

386.4
MW (Da)
3.61
ALogP
4
HBA
0
HBD
50.5
PSA (Ų)
0.63
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H19FN4O
MW 386.43
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.11

Activity Summary

Ki 4 meas. best 5.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-5
CHEMBL5112
Ki 5.3 5.3 5000.0 1
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL4956
Ki 4.52 4.52 30000.0 1
Gamma-aminobutyric acid receptor subunit alpha-1
CHEMBL1962
Ki 4.26 4.26 55000.0 1
Gamma-aminobutyric acid receptor subunit alpha-3
CHEMBL3026
Ki 4.2 4.2 63000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31738537 10.1021/acs.jmedchem.9b01312 Unchecked 3
31738537 10.1021/acs.jmedchem.9b01312 Gamma-aminobutyric acid receptor subunit alpha-1 2
31738537 10.1021/acs.jmedchem.9b01312 Gamma-aminobutyric acid receptor subunit alpha-2 2
31738537 10.1021/acs.jmedchem.9b01312 Gamma-aminobutyric acid receptor subunit alpha-3 2
31738537 10.1021/acs.jmedchem.9b01312 Gamma-aminobutyric acid receptor subunit alpha-5 2

Data from ChEMBL 36 via Core Engine