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Compound Detail

CHEMBL13458

RO-052921
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O=C1CN=C(c2ccccc2)c2ccccc2N1

Basic Information

ChEMBL ID CHEMBL13458
Name RO-052921
Phase Preclinical
Structure Type MOL
InChI Key IVUAAOBNUNMJQC-UHFFFAOYSA-N

Known Names

Ro-052921
8
Targets
10
Activities
2
Assay Types
0
PK Parameters
20
Publications
1
Known Names

Molecular Properties

236.3
MW (Da)
2.48
ALogP
2
HBA
1
HBD
41.5
PSA (Ų)
0.81
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H12N2O
MW 236.27
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.14

Activity Summary

Ki 8 meas. best 6.85
IC50 2 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 6.85 6.85 140.0 1
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2
CHEMBL4523641
Ki 6.85 6.85 140.0 1
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 6.63 6.63 233.0 1
GABA A receptor alpha-2/beta-2/gamma-2
CHEMBL2111413
Ki 6.63 6.63 233.0 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 6.54 6.54 286.0 1
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
Ki 6.54 6.54 288.0 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 6.46 6.46 350.0 1
GABA A receptor alpha-3/beta-2/gamma-2
CHEMBL2111339
Ki 6.46 6.46 350.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28109947 10.1016/j.ejmech.2016.12.032 Unchecked 12
7381845 10.1021/jm00178a018 ADMET 5
926122 10.1021/jm00219a019 Mus musculus 4
28259528 10.1016/j.bmc.2017.02.020 Histone deacetylase 8 2
28109947 10.1016/j.ejmech.2016.12.032 Histone deacetylase 8 2
28109947 10.1016/j.ejmech.2016.12.032 Histone deacetylase 6 2
28109947 10.1016/j.ejmech.2016.12.032 Histone deacetylase 3 2
28109947 10.1016/j.ejmech.2016.12.032 Histone deacetylase 1 2
926122 10.1021/jm00219a019 Felis catus 2
2202830 10.1021/jm00171a037 Unchecked 2
35218882 10.1016/j.bmcl.2022.128637 Unchecked 1
8978853 10.1021/jm960536o Translocator protein 1
21306904 10.1016/j.bmc.2011.01.010 Trypanosoma brucei brucei 1
10633039 10.1021/jm990341r Unchecked 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-6/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-5/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-3/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-2/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-1/beta-3/gamma-2 1
6876077 10.1021/jm00362a003 Mus musculus 1

Data from ChEMBL 36 via Core Engine