Target
Runt-related transcription factor 1
Ligand
BDBM29650
Substrate
Venus-CBFbeta-SMMHC
Meas. Tech.
uHTS identification of compounds inhibiting the binding between the RUNX1 Runt domain and CBFb-SMMHC via a fluorescence resonance energy transfer (FRET) assay.
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
100000±n/a nM
Citation
 PubChem, PC uHTS identification of compounds inhibiting the binding between the RUNX1 Runt domain and CBFbeta-SMMHC via a fluorescence resonance energy transfer (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:
BDBM29650
Synonyms:
1-Benzyl-2-[(5-bromo-furan-2-carbonyl)-amino]-1H-pyrrolo[2,3-b]quinoxaline-3-carboxylic acid (2-methoxy-ethyl)-amide | 1-benzyl-2-[(5-bromo-2-furoyl)amino]-N-(2-methoxyethyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide | 1-benzyl-2-[(5-bromofuran-2-carbonyl)amino]-N-(2-methoxyethyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide | 2-[(5-bromanylfuran-2-yl)carbonylamino]-N-(2-methoxyethyl)-1-(phenylmethyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide | 2-[[(5-bromo-2-furanyl)-oxomethyl]amino]-N-(2-methoxyethyl)-1-(phenylmethyl)-3-pyrrolo[3,2-b]quinoxalinecarboxamide | MLS000556283 | SMR000147600 | cid_1925701
Type:
Small organic molecule
Emp. Form.:
C26H22BrN5O4
Mol. Mass.:
548.388
SMILES:
COCCNC(=O)c1c(NC(=O)c2ccc(Br)o2)n(Cc2ccccc2)c2nc3ccccc3nc12
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