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Target
Runt-related transcription factor 1
Ligand
BDBM29688
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
14600±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:
BDBM29688
Synonyms:
3-(9-(3-chloro-4-{[(4-methylphenyl)sulfonyl]oxy}phenyl)-1,8-dioxo-2,3,4,5,6,7,8,9-octahydro-10(1H)-acridinyl)propanoic acid | 3-[9-(3-chloro-4-tosyloxy-phenyl)-1,8-diketo-3,4,5,6,7,9-hexahydro-2H-acridin-10-yl]propionic acid | 3-[9-[3-chloranyl-4-(4-methylphenyl)sulfonyloxy-phenyl]-1,8-bis(oxidanylidene)-3,4,5,6,7,9-hexahydro-2H-acridin-10-yl]propanoic acid | 3-[9-[3-chloro-4-(4-methylphenyl)sulfonyloxyphenyl]-1,8-dioxo-3,4,5,6,7,9-hexahydro-2H-acridin-10-yl]propanoic acid | MLS000704358 | SMR000230917 | cid_1770167
Type:
Small organic molecule
Emp. Form.:
C29H28ClNO7S
Mol. Mass.:
570.053
SMILES:
Cc1ccc(cc1)S(=O)(=O)Oc1ccc(cc1Cl)C1C2=C(CCCC2=O)N(CCC(O)=O)C2=C1C(=O)CCC2 |c:35,t:21|
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