Reaction Details Report a problem with these data
Target
Bromodomain-containing protein 8
Ligand
BDBM220447
Substrate
n/a
Meas. Tech.
ChEMBL_1670382 (CHEMBL4020270)
Kd
>1000±n/a nM
Citation
 McDaniel, KF; Wang, L; Soltwedel, T; Fidanze, SD; Hasvold, LA; Liu, D; Mantei, RA; Pratt, JK; Sheppard, GS; Bui, MH; Faivre, EJ; Huang, X; Li, L; Lin, X; Wang, R; Warder, SE; Wilcox, D; Albert, DH; Magoc, TJ; Rajaraman, G; Park, CH; Hutchins, CW; Shen, JJ; Edalji, RP; Sun, CC; Martin, R; Gao, W; Wong, S; Fang, G; Elmore, SW; Shen, Y; Kati, WM Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor. J Med Chem 60:8369-8384 (2017) [PubMed]  Article 
Target
Name:
Bromodomain-containing protein 8
Synonyms:
BRD8 | BRD8_HUMAN | Bromodomain-containing protein 8 | SMAP | SMAP | SMAP2 | Skeletal muscle abundant protein | Skeletal muscle abundant protein 2 | Thyroid hormone receptor coactivating protein of 120 kDa | TrCP120 | p120
Type:
PROTEIN
Mol. Mass.:
135233.03
Organism:
Homo sapiens (Human)
Description:
ChEMBL_109820
Residue:
1235
Sequence:
MATGTGKHKLLSTGPTEPWSIREKLCLASSVMRSGDQNWVSVSRAIKPFAEPGRPPDWFSQKHCASQYSELLETTETPKRKRGEKGEVVETVEDVIVRKLTAERVEELKKVIKETQERYRRLKRDAELIQAGHMDSRLDELCNDIATKKKLEEEEAEVKRKATDAAYQARQAVKTPPRRLPTVMVRSPIDSASPGGDYPLGDLTPTTMEEATSGVNESEMAVASGHLNSTGVLLEVGGVLPMIHGGEIQQTPNTVAASPAASGAPTLSRLLEAGPTQFTTPLASFTTVASEPPVKLVPPPVESVSQATIVMMPALPAPSSAPAVSTTESVAPVSQPDNCVPMEAVGDPHTVTVSMDSSEISMIINSIKEECFRSGVAEAPVGSKAPSIDGKEELDLAEKMDIAVSYTGEELDFETVGDIIAIIEDKVDDHPEVLDVAAVEAALSFCEENDDPQSLPGPWEHPIQQERDKPVPLPAPEMTVKQERLDFEETENKGIHELVDIREPSAEIKVEPAEPEPVISGAEIVAGVVPATSMEPPELRSQDLDEELGSTAAGEIVEADVAIGKGDETPLTNVKTEASPESMLSPSHGSNPIEDPLEAETQHKFEMSDSLKEESGTIFGSQIKDAPGEDEEEDGVSEAASLEEPKEEDQGEGYLSEMDNEPPVSESDDGFSIHNATLQSHTLADSIPSSPASSQFSVCSEDQEAIQAQKIWKKAIMLVWRAAANHRYANVFLQPVTDDIAPGYHSIVQRPMDLSTIKKNIENGLIRSTAEFQRDIMLMFQNAVMYNSSDHDVYHMAVEMQRDVLEQIQQFLATQLIMQTSESGISAKSLRGRDSTRKQDASEKDSVPMGSPAFLLSLFMGHEWVWLDSEQDHPNDSELSNDCRSLFSSWDSSLDLDVGNWRETEDPEAEELEESSPEREPSELLVGDGGSEESQEAARKASHQNLLHFLSEVAYLMEPLCISSNESSEGCCPPSGTRQEGREIKASEGERELCRETEELSAKGDPLVAEKPLGENGKPEVASAPSVICTVQGLLTESEEGEAQQESKGEDQGEVYVSEMEDQPPSGECDDAFNIKETPLVDTLFSHATSSKLTDLSQDDPVQDHLLFKKTLLPVWKMIASHRFSSPFLKPVSERQAPGYKDVVKRPMDLTSLKRNLSKGRIRTMAQFLRDLMLMFQNAVMYNDSDHHVYHMAVEMRQEVLEQIQVLNIWLDKRKGSSSLEGEPANPVDDGKPVF
  
Inhibitor
Name:
BDBM220447
Synonyms:
US10633379, Compound X | US9296741, 36
Type:
Small organic molecule
Emp. Form.:
C22H19F2N3O4S
Mol. Mass.:
459.466
SMILES:
CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(c1)-c1cn(C)c(=O)c2[nH]ccc12
Structure:
Search PDB for entries with ligand similarity: