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Target
Runt-related transcription factor 1
Ligand
BDBM29617
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
57500±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:
BDBM29617
Synonyms:
2-azanylidene-1-(furan-2-ylmethyl)-3-(phenylsulfonyl)dipyrido[1,2-d:3',4'-f]pyrimidin-5-one | 3-(benzenesulfonyl)-1-(2-furanylmethyl)-2-imino-5-dipyrido[1,2-d:3',4'-f]pyrimidinone | 3-(benzenesulfonyl)-1-(furan-2-ylmethyl)-2-iminodipyrido[1,2-d:3',4'-f]pyrimidin-5-one | 3-Benzenesulfonyl-1-furan-2-ylmethyl-2-imino-1,2-dihydro-1,9,10a-triaza-anthracen-10-one | 3-besyl-1-(2-furfuryl)-2-imino-dipyrido[1,2-d:3',4'-f]pyrimidin-5-one | MLS000033902 | SMR000013661 | cid_656318
Type:
Small organic molecule
Emp. Form.:
C22H16N4O4S
Mol. Mass.:
432.452
SMILES:
N=c1c(cc2c(nc3ccccn3c2=O)n1Cc1ccco1)S(=O)(=O)c1ccccc1
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