5-{4-[2-(Methyl-pyridin-2-yl-amino)-ethoxy]-benzyl}-thiazolidine-2,4-dione

ID: ALA121

Chembl Id: CHEMBL121

Max Phase: Approved

First Approval: 1999

Molecular Formula: C18H19N3O3S

Molecular Weight: 357.44

Molecule Type: Small molecule

Names and Identifiers

Synonyms: Avandamet | Avandaryl | Avandia | Gaudil | Rezult | Rosiglitazone | Rosiglizole | Rosvel | BRL-49653 | NSC-758698 | TDZ-01

Synonyms from Alternative Forms(7): Rosiglitazone maleate | Avandia | Rosiglitzazone maleate | BRL-49653 | BRL-49653-C | BRL-49653C | NSC-717764

Trade Names(1): Avandia

Canonical SMILES:  CN(CCOc1ccc(CC2SC(=O)NC2=O)cc1)c1ccccn1

Standard InChI:  InChI=1S/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23)

Standard InChI Key:  YASAKCUCGLMORW-UHFFFAOYSA-N

Alternative Forms

1. Parent:

   

   ALA121

   ROSIGLITAZONE

2. Alternative Forms:

   

   ALA121

   Rosiglitazone maleate
3. 

   ALA121

   Rosiglitazone HCl

Molecule Features

Natural Product: Yes

Oral: Yes

Chemical Probe: No

Parenteral: No

Molecule Type: Small molecule

Topical: No

First In Class: No

Black Box: Yes

Chirality: No

Availability: No

Prodrug: No

Calculated Properties

Molecular Weight: 357.44

Molecular Weight (Monoisotopic): 357.1147

AlogP: 2.49

#Rotatable Bonds: 7

Polar Surface Area: 71.53

Molecular Species: NEUTRAL

HBA: 6

HBD: 1

#RO5 Violations: ┄

HBA (Lipinski): 6

HBD (Lipinski): 1

#RO5 Violations (Lipinski): ┄

CX Acidic pKa: 6.84

CX Basic pKa: 6.23

CX LogP: 2.45

CX LogD: 2.21

Aromatic Rings: 2

Heavy Atoms: 25

QED Weighted: 0.82

Np Likeness Score: -0.93

References

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289. Unpublished dataset, 

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Source

Source(17):

• Scientific Literature
• PubChem BioAssays
• Clinical Candidates
• DrugMatrix
• TP-search Transporter Database
• Deposited Supplementary Bioactivity Data
• AstraZeneca Deposited Data
• Withdrawn Drugs
• BindingDB Database
• Patent Bioactivity Data
• WHO Anatomical Therapeutic Chemical Classification
• British National Formulary
• SARS-CoV-2 Screening Data 2020-21
• EUbOPEN Chemogenomic Library
• IMI-CARE SARS-CoV-2 Data
• Fraunhofer HDAC6
• Zimmerman Lab Biotransformation data Dec 2023