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Target
Runt-related transcription factor 1
Ligand
BDBM29627
Substrate
Venus-CBFbeta-SMMHC
Meas. Tech.
Identification of compounds inhibiting the binding between the RUNX1 Runt domain and CBFbeta-SMMHC via a time resolved fluorescence resonance energy transfer (TR-FRET) assay.
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
43500±n/a nM
Citation
 PubChem, PC Identification of compounds inhibiting the binding between the RUNX1 Runt domain and CBFb-SMMHC via a time resolved fluorescence resonance energy transfer (TR-FRET) assay. PubChem Bioassay (2009)[AID]
Target
Name:
Runt-related transcription factor 1
Synonyms:
AML1 | Acute myeloid leukemia 1 protein | CBF-alpha-2 | CBFA2 | Core-binding factor subunit alpha-2 | Oncogene AML-1 | Polyomavirus enhancer-binding protein 2 alpha B subunit | RUNX1 | RUNX1_HUMAN | Runt-Related Transcription Factor 1 Isoform AML1C
Type:
Subunit of heterodimeric transcription factor
Mol. Mass.:
48750.25
Organism:
Homo sapiens (Human)
Description:
Q01196
Residue:
453
Sequence:
MRIPVDASTSRRFTPPSTALSPGKMSEALPLGAPDAGAALAGKLRSGDRSMVEVLADHPGELVRTDSPNFLCSVLPTHWRCNKTLPIAFKVVALGDVPDGTLVTVMAGNDENYSAELRNATAAMKNQVARFNDLRFVGRSGRGKSFTLTITVFTNPPQVATYHRAIKITVDGPREPRRHRQKLDDQTKPGSLSFSERLSELEQLRRTAMRVSPHHPAPTPNPRASLNHSTAFNPQPQSQMQDTRQIQPSPPWSYDQSYQYLGSIASPSVHPATPISPGRASGMTTLSAELSSRLSTAPDLTAFSDPRQFPALPSISDPRMHYPGAFTYSPTPVTSGIGIGMSAMGSATRYHTYLPPPYPGSSQAQGGPFQASSPSYHLYYGASAGSYQFSMVGGERSPPRILPPCTNASTGSALLNPSLPNQSDVVEAEGSHSNSPTNMAPSARLEEAVWRPY
  
Inhibitor
Name:
BDBM29627
Synonyms:
2-azanylidene-N-[(4-fluorophenyl)methyl]-1-(furan-2-ylmethyl)-5-oxidanylidene-dipyrido[1,2-d:3',4'-f]pyrimidine-3-carboxamide | MLS000040311 | N-(4-fluorobenzyl)-1-(2-furfuryl)-2-imino-5-keto-dipyrido[1,2-d:3',4'-f]pyrimidine-3-carboxamide | N-[(4-fluorophenyl)methyl]-1-(2-furanylmethyl)-2-imino-5-oxo-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxamide | N-[(4-fluorophenyl)methyl]-1-(furan-2-ylmethyl)-2-imino-5-oxodipyrido[1,2-d:3',4'-f]pyrimidine-3-carboxamide | SMR000045850 | cid_664843
Type:
Small organic molecule
Emp. Form.:
C24H18FN5O3
Mol. Mass.:
443.4298
SMILES:
Fc1ccc(CNC(=O)c2cc3c(nc4ccccn4c3=O)n(Cc3ccco3)c2=N)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Core-binding factor subunit beta isoform 2
Synonyms:
CBFB | CBFbeta | PEBB_HUMAN | Venus-CBFbeta-SMMHC | Venus-core-binding factor subunit beta-smooth muscle myosin heavy chain
Type:
Fluorescent fusion protein
Mol. Mass.:
21988.19
Organism:
Homo sapiens (Human)
Description:
Q13951-2
Residue:
187
Sequence:
MPRVVPDQRSKFENEEFFRKLSRECEIKYTGFRDRPHEERQARFQNACRDGRSEIAFVATGTNLSLQFFPASWQGEQRQTPSREYVDLEREAGKVYLKAPMILNGVCVIWKGWIDLQRLDGMGCLEFDEERAQQEDALAQQAFEEARRRTREFEDRDRSHREEMEARRQQDPSPGSNLGGGDDLKLR