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Compound Detail

CHEMBL4071696

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[2H]C([2H])(C)OC(=O)c1ncn2c1CN=C(c1ccccn1)c1cc(C#C)ccc1-2

Basic Information

ChEMBL ID CHEMBL4071696
Phase Preclinical
Structure Type MOL
InChI Key ZSEDMNMFODMQRD-APZFVMQVSA-N
Parent Compound CHEMBL475022
Active Moiety CHEMBL475022
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

356.4
MW (Da)
2.78
ALogP
6
HBA
0
HBD
69.4
PSA (Ų)
0.53
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16N4O2
MW 358.40
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.88

Activity Summary

EC50 1 meas. best 5.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
EC50 5.93 5.93 1170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27933953 10.1021/acs.jmedchem.6b01332 Plasma 4
27933953 10.1021/acs.jmedchem.6b01332 Liver 3
27933953 10.1021/acs.jmedchem.6b01332 Brain 2
27933953 10.1021/acs.jmedchem.6b01332 HEK-293T 1
27933953 10.1021/acs.jmedchem.6b01332 GABA-A receptor; alpha-3/beta-3/gamma-2 1
27933953 10.1021/acs.jmedchem.6b01332 GABA-A receptor; alpha-1/beta-3/gamma-2 1
27933953 10.1021/acs.jmedchem.6b01332 Mus musculus 1

Data from ChEMBL 36 via Core Engine