Reaction Details Report a problem with these data
Target
Runt-related transcription factor 1
Ligand
BDBM31176
Substrate
Venus-CBFbeta-SMMHC
Meas. Tech.
FRET Assay
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
18500±3500 nM
Citation
Gorczynski, MJ; Grembecka, J; Zhou, Y; Kong, Y; Roudaia, L; Douvas, MG; Newman, M; Bielnicka, I; Baber, G; Corpora, T; Shi, J; Sridharan, M; Lilien, R; Donald, BR; Speck, NA; Brown, ML; Bushweller, JH Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta. Chem Biol 14:1186-97 (2007) [PubMed] Article
More Info.:
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:
BDBM31176
Synonyms:
thiazol-2-amine, 6
Type:
Small organic molecule
Emp. Form.:
C10H10N2OS
Mol. Mass.:
206.264
SMILES:
COc1ccc(cc1)-c1csc(N)n1
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