Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL523

NORDAZEPAM
🧪 Phase II
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
🧪 Phase II
O=C1CN=C(c2ccccc2)c2cc(Cl)ccc2N1

Basic Information

ChEMBL ID CHEMBL523
Name NORDAZEPAM
Phase Phase II
Structure Type MOL
InChI Key AKPLHCDWDRPJGD-UHFFFAOYSA-N

Known Names

Calmday Demadar Desmethyldiazepam Desoxydemoxepam Madar N-desmethyldiazepam Nordazepam Nordazepam civ Nordiazepam NSC-46078 NSC-631619 Praxadium +3 more
1
Targets
7
Activities
2
Assay Types
8
PK Parameters
20
Publications
15
Known Names
1
Indications

Molecular Properties

270.7
MW (Da)
3.13
ALogP
2
HBA
1
HBD
41.5
PSA (Ų)
0.85
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Natural Product
USAN Stem -azepam

Extended Properties

Molecular Formula C15H11ClN2O
MW 270.72
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.51

Indications

Anxiety

ATC Classification

N05BA16
nordazepam
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS

Activity Summary

IC50 6 meas.
Ki 1 meas. best 4.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL2094133
Ki 4.14 4.14 73000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.12 mL.min-1.kg-1 Homo sapiens
F 80.0 % Homo sapiens
F 99.0 % Homo sapiens
Fu 0.03 - Homo sapiens
Fu 0.03 - Homo sapiens
MRT 63.0 hr Homo sapiens
T1/2 46.0 hr Homo sapiens
T1/2 50.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-A receptor; anion channel Ki = 73000.0 nM 4.14 Binding affinity for umolar GABA-A central benzodiazepine receptor 6330354

Literature References

PubMed DOI Target Context # Activities
31483 10.1021/jm00210a022 Mus musculus 11
6330354 10.1021/jm00372a012 Mus musculus 6
7381845 10.1021/jm00178a018 ADMET 5
18426954 10.1124/dmd.108.020479 ADMET 4
926122 10.1021/jm00219a019 Mus musculus 4
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 4
11384238 10.1021/jm001101a Homo sapiens 3
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 3
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 3
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 3
7359533 10.1021/jm00176a016 Rattus norvegicus 3
2202830 10.1021/jm00171a037 Unchecked 3
26550826 10.1038/nature15699 C-X-C chemokine receptor type 4 2
37468498 10.1038/s41467-023-40064-9 Histamine H2 receptor 2
18524583 10.1016/j.bmcl.2008.05.065 Hepatitis B virus 2
9171882 10.1021/jm960592p D341 cell line 2
12438524 10.1124/jpet.102.039255 ATP-dependent translocase ABCB1 2

Data from ChEMBL 36 via Core Engine