Target
Runt-related transcription factor 1
Ligand
BDBM29658
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
6540±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:
BDBM29658
Synonyms:
MLS000557330 | N-[3-Cyano-1-furan-2-ylmethyl-8-methyl-10-oxo-1,10-dihydro-1,9,10a-triaza-anthracen-(2Z)-ylidene]-3- methyl-benzamide | N-[3-cyano-1-(2-furanylmethyl)-10-methyl-5-oxo-2-dipyrido[3,4-c:1',2'-f]pyrimidinylidene]-3-methylbenzamide | N-[3-cyano-1-(2-furfuryl)-5-keto-10-methyl-dipyrido[3,4-c:1',2'-f]pyrimidin-2-ylidene]-3-methyl-benzamide | N-[3-cyano-1-(furan-2-ylmethyl)-10-methyl-5-oxidanylidene-dipyrido[3,4-c:1',2'-f]pyrimidin-2-ylidene]-3-methyl-benzamide | N-[3-cyano-1-(furan-2-ylmethyl)-10-methyl-5-oxodipyrido[3,4-c:1',2'-f]pyrimidin-2-ylidene]-3-methylbenzamide | SMR000148247 | cid_4522020
Type:
Small organic molecule
Emp. Form.:
C26H19N5O3
Mol. Mass.:
449.4608
SMILES:
Cc1cccc(c1)C(=O)\N=c1/c(cc2c(nc3c(C)cccn3c2=O)n1Cc1ccco1)C#N
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