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Target
Bromodomain-containing protein 3
Ligand
BDBM264435
Substrate
n/a
Meas. Tech.
TR-FRET In-Vitro Binding Assays for BRD2, BRD3, and BRD4
pH
7.5±n/a
IC50
82.0±n/a nM
Comments
extracted
Citation
 Blank, J; Cotesta, S; Guagnano, V; Rueeger, H Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease US Patent  US9714249 Publication Date 7/25/2017 
Target
Name:
Bromodomain-containing protein 3
Synonyms:
BRD3 | BRD3_HUMAN | Bromodomain and extra-terminal motif (BET) | Bromodomain-containing protein 3 | Bromodomain-containing protein 3 (BRD3) | KIAA0043 | RING3-like protein | RING3L
Type:
Protein
Mol. Mass.:
79571.81
Organism:
Homo sapiens (Human)
Description:
Q15059
Residue:
726
Sequence:
MSTATTVAPAGIPATPGPVNPPPPEVSNPSKPGRKTNQLQYMQNVVVKTLWKHQFAWPFYQPVDAIKLNLPDYHKIIKNPMDMGTIKKRLENNYYWSASECMQDFNTMFTNCYIYNKPTDDIVLMAQALEKIFLQKVAQMPQEEVELLPPAPKGKGRKPAAGAQSAGTQQVAAVSSVSPATPFQSVPPTVSQTPVIAATPVPTITANVTSVPVPPAAAPPPPATPIVPVVPPTPPVVKKKGVKRKADTTTPTTSAITASRSESPPPLSDPKQAKVVARRESGGRPIKPPKKDLEDGEVPQHAGKKGKLSEHLRYCDSILREMLSKKHAAYAWPFYKPVDAEALELHDYHDIIKHPMDLSTVKRKMDGREYPDAQGFAADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPVEAPALPAPAAPMVSKGAESSRSSEESSSDSGSSDSEEERATRLAELQEQLKAVHEQLAALSQAPVNKPKKKKEKKEKEKKKKDKEKEKEKHKVKAEEEKKAKVAPPAKQAQQKKAPAKKANSTTTAGRQLKKGGKQASASYDSEEEEEGLPMSYDEKRQLSLDINRLPGEKLGRVVHIIQSREPSLRDSNPDEIEIDFETLKPTTLRELERYVKSCLQKKQRKPFSASGKKQAAKSKEELAQEKKKELEKRLQDVSGQLSSSKKPARKEKPGSAPSGGPSRLSSSSSSESGSSSSSGSSSDSSDSE
  
Inhibitor
Name:
BDBM264435
Synonyms:
6-(4-chlorophenyl)-3-cyclopropyl-5-(1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)-1-(1-methyl-1H-pyrazol-5-yl)-5,6-dihydropyrrolo[3,4-c]pyrazol-4(1H)-one | US9714249, 5
Type:
Small organic molecule
Emp. Form.:
C25H25ClN6O2
Mol. Mass.:
476.958
SMILES:
Cc1cc(cn(C)c1=O)N1C(C(Nc2ccnn2C)=C(C(=N)C2CC2)C1=O)c1ccc(Cl)cc1 |t:20|
Structure:
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