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Target
DNA topoisomerase 1
Ligand
BDBM50034015
Substrate
n/a
Meas. Tech.
ChEMBL_53721 (CHEMBL663649)
IC50
167±n/a nM
Citation
Uehling, DE; Nanthakumar, SS; Croom, D; Emerson, DL; Leitner, PP; Luzzio, MJ; McIntyre, G; Morton, B; Profeta, S; Sisco, J Synthesis, topoisomerase I inhibitory activity, and in vivo evaluation of 11-azacamptothecin analogs. J Med Chem 38:1106-18 (1995) [PubMed] Article
More Info.:
Target
Name:
DNA topoisomerase 1
Synonyms:
DNA topoisomerase I | DNA topoisomerase I (Topo I) | TOP1 | TOP1_HUMAN
Type:
Enzyme
Mol. Mass.:
90771.02
Organism:
Human
Description:
P11387
Residue:
765
Sequence:
MSGDHLHNDSQIEADFRLNDSHKHKDKHKDREHRHKEHKKEKDREKSKHSNSEHKDSEKKHKEKEKTKHKDGSSEKHKDKHKDRDKEKRKEEKVRASGDAKIKKEKENGFSSPPQIKDEPEDDGYFVPPKEDIKPLKRPRDEDDADYKPKKIKTEDTKKEKKRKLEEEEDGKLKKPKNKDKDKKVPEPDNKKKKPKKEEEQKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKFYYDGKVMKLSPKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLSKCDFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKERIANFKIEPPGLFRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPGHKWKEVRHDNKVTWLVSWTENIQGSIKYIMLNPSSRIKGEKDWQKYETARRLKKCVDKIRNQYREDWKSKEMKVRQRAVALYFIDKLALRAGNEKEEGETADTVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNKVPVEKRVFKNLQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITLQQQLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQTKIDAKKEQLADARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQLMKLEVQATDREENKQIALGTSKLNYLDPRITVAWCKKWGVPIEKIYNKTQREKFAWAIDMADEDYEF
Inhibitor
Name:
BDBM50034015
Synonyms:
(S)-9-Aminomethyl-4,11-diethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,8,12a-triaza-dibenzo[b,h]fluorene-3,13-dione | CHEMBL13848
Type:
Small organic molecule
Emp. Form.:
C22H22N4O4
Mol. Mass.:
406.4345
SMILES:
CCc1c2Cn3c(cc4c(COC(=O)[C@]4(O)CC)c3=O)-c2nc2cnc(CN)cc12