Target
Runt-related transcription factor 1
Ligand
BDBM29686
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
19600±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:
BDBM29686
Synonyms:
(7-hydroxy-2-oxochromen-4-yl)methyl 2-(3-oxo-4H-1,4-benzothiazin-2-yl)acetate | (7-oxidanyl-2-oxidanylidene-chromen-4-yl)methyl 2-(3-oxidanylidene-4H-1,4-benzothiazin-2-yl)ethanoate | 2-(3-keto-4H-1,4-benzothiazin-2-yl)acetic acid (7-hydroxy-2-keto-chromen-4-yl)methyl ester | 2-(3-oxo-4H-1,4-benzothiazin-2-yl)acetic acid (7-hydroxy-2-oxo-1-benzopyran-4-yl)methyl ester | MLS000393940 | SMR000247371 | cid_5853681
Type:
Small organic molecule
Emp. Form.:
C20H15NO6S
Mol. Mass.:
397.401
SMILES:
Oc1ccc2c(COC(=O)CC3Sc4ccccc4NC3=O)cc(=O)oc2c1
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