Molecule Details
InChIKeyRJURFGZVJUQBHK-IIXSONLDSA-N
Canonical SMILESCc1c2oc3c(C)ccc(C(=O)N[C@@H]4C(=O)N[C@H](C(C)C)C(=O)N5CCC[C@H]5C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]4C)c3nc-2c(C(=O)N[C@@H]2C(=O)N[C@H](C(C)C)C(=O)N3CCC[C@H]3C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]2C)c(N)c1=O
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Cross-Family
Avg pChEMBL7.09
SourceBindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB00970
Drug NameDactinomycin
CAS Number50-76-0
Groups approved investigational
ATC Codes L01DA01
DescriptionA compound composed of a two cyclic peptides attached to a phenoxazine that is derived from streptomyces parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, prot...

Categories: Actinomycin Actinomycines Amino Acids, Peptides, and Proteins Anti-Infective Agents Antibiotics, Antineoplastic Antineoplastic Agents Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Substrates Cytotoxic Antibiotics and Related Substances Cytotoxins Enzyme Inhibitors Heterocyclic Compounds, Fused-Ring Immunosuppressive Agents Myelosuppressive Agents Narrow Therapeutic Index Drugs Nucleic Acid Synthesis Inhibitors P-glycoprotein inhibitors P-glycoprotein substrates P-glycoprotein substrates with a Narrow Therapeutic Index Peptides Peptides, Cyclic Protein Synthesis Inhibitors
Cross-references: BindingDB: 50089528 ChEBI: 27666 CHEMBL1554 ChemSpider: 10482167 Drugs Product Database (DPD): 8486 C06770 D00214 PharmGKB: PA151917012 PubChem:457193 PubChem:46509192 RxCUI: 3100 Therapeutic Targets Database: DNC000380 Wikipedia: Dactinomycin
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P41543 OST1 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) Pathogen PF04597 7.4 Ki BindingDB
P0A8T7 rpoC Escherichia coli (strain K12) Pathogen PF04997 PF00623 PF04983 PF05000 PF04998 6.8 IC50 BindingDB
DrugBank Target Actions (8)
Target Gene Target Name Action Type
P11387 TOP1 DNA topoisomerase 1 inhibitor targets
P11388 TOP2A DNA topoisomerase 2 inhibitor targets
O76082 O76082 Organic cation/carnitine transporter 2 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
O95255 O95255 ATP-binding cassette sub-family C member 6 substrate transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters
P33527 ABCC1 Multidrug resistance-associated protein 1 substrate transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 substrate transporters