Reaction Details |
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Target | Bromodomain adjacent to zinc finger domain protein 2A |
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Ligand | BDBM50028142 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1434736 (CHEMBL3383405) |
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IC50 | <31623±n/a nM |
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Citation | Gosmini, R; Nguyen, VL; Toum, J; Simon, C; Brusq, JM; Krysa, G; Mirguet, O; Riou-Eymard, AM; Boursier, EV; Trottet, L; Bamborough, P; Clark, H; Chung, CW; Cutler, L; Demont, EH; Kaur, R; Lewis, AJ; Schilling, MB; Soden, PE; Taylor, S; Walker, AL; Walker, MD; Prinjha, RK; Nicodème, E The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem57:8111-31 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Bromodomain adjacent to zinc finger domain protein 2A |
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Name: | Bromodomain adjacent to zinc finger domain protein 2A |
Synonyms: | BAZ2A | BAZ2A_HUMAN | Bromodomain adjacent to zinc finger domain protein 2A | KIAA0314 | KIAA0314 | TIP5 | TTF-I-interacting protein 5 | Transcription termination factor I-interacting protein 5 | hWALp3 |
Type: | PROTEIN |
Mol. Mass.: | 211197.21 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_108002 |
Residue: | 1905 |
Sequence: | MEMEANDHFNFTGLPPAPAASGLKPSPSSGEGLYTNGSPMNFPQQGKSLNGDVNVNGLST
VSHTTTSGILNSAPHSSSTSHLHHPSVAYDCLWNYSQYPSANPGSNLKDPPLLSQFSGGQ
YPLNGILGGSRQPSSPSHNTNLRAGSQEFWANGTQSPMGLNFDSQELYDSFPDQNFEVMP
NGPPSFFTSPQTSPMLGSSIQTFAPSQEVGSGIHPDEAAEKEMTSVVAENGTGLVGSLEL
EEEQPELKMCGYNGSVPSVESLHQEVSVLVPDPTVSCLDDPSHLPDQLEDTPILSEDSLE
PFNSLAPEPVSGGLYGIDDTELMGAEDKLPLEDSPVISALDCPSLNNATAFSLLADDSQT
STSIFASPTSPPVLGESVLQDNSFDLNNGSDAEQEEMETQSSDFPPSLTQPAPDQSSTIQ
LHPATSPAVSPTTSPAVSLVVSPAASPEISPEVCPAASTVVSPAVFSVVSPASSAVLPAV
SLEVPLTASVTSPKASPVTSPAAAFPTASPANKDVSSFLETTADVEEITGEGLTASGSGD
VMRRRIATPEEVRLPLQHGWRREVRIKKGSHRWQGETWYYGPCGKRMKQFPEVIKYLSRN
VVHSVRREHFSFSPRMPVGDFFEERDTPEGLQWVQLSAEEIPSRIQAITGKRGRPRNTEK
AKTKEVPKVKRGRGRPPKVKITELLNKTDNRPLKKLEAQETLNEEDKAKIAKSKKKMRQK
VQRGECQTTIQGQARNKRKQETKSLKQKEAKKKSKAEKEKGKTKQEKLKEKVKREKKEKV
KMKEKEEVTKAKPACKADKTLATQRRLEERQRQQMILEEMKKPTEDMCLTDHQPLPDFSR
VPGLTLPSGAFSDCLTIVEFLHSFGKVLGFDPAKDVPSLGVLQEGLLCQGDSLGEVQDLL
VRLLKAALHDPGFPSYCQSLKILGEKVSEIPLTRDNVSEILRCFLMAYGVEPALCDRLRT
QPFQAQPPQQKAAVLAFLVHELNGSTLIINEIDKTLESMSSYRKNKWIVEGRLRRLKTVL
AKRTGRSEVEMEGPEECLGRRRSSRIMEETSGMEEEEEEESIAAVPGRRGRRDGEVDATA
SSIPELERQIEKLSKRQLFFRKKLLHSSQMLRAVSLGQDRYRRRYWVLPYLAGIFVEGTE
GNLVPEEVIKKETDSLKVAAHASLNPALFSMKMELAGSNTTASSPARARGRPRKTKPGSM
QPRHLKSPVRGQDSEQPQAQLQPEAQLHAPAQPQPQLQLQLQSHKGFLEQEGSPLSLGQS
QHDLSQSAFLSWLSQTQSHSSLLSSSVLTPDSSPGKLDPAPSQPPEEPEPDEAESSPDPQ
ALWFNISAQMPCNAAPTPPPAVSEDQPTPSPQQLASSKPMNRPSAANPCSPVQFSSTPLA
GLAPKRRAGDPGEMPQSPTGLGQPKRRGRPPSKFFKQMEQRYLTQLTAQPVPPEMCSGWW
WIRDPEMLDAMLKALHPRGIREKALHKHLNKHRDFLQEVCLRPSADPIFEPRQLPAFQEG
IMSWSPKEKTYETDLAVLQWVEELEQRVIMSDLQIRGWTCPSPDSTREDLAYCEHLSDSQ
EDITWRGRGREGLAPQRKTTNPLDLAVMRLAALEQNVERRYLREPLWPTHEVVLEKALLS
TPNGAPEGTTTEISYEITPRIRVWRQTLERCRSAAQVCLCLGQLERSIAWEKSVNKVTCL
VCRKGDNDEFLLLCDGCDRGCHIYCHRPKMEAVPEGDWFCTVCLAQQVEGEFTQKPGFPK
RGQKRKSGYSLNFSEGDGRRRRVLLRGRESPAAGPRYSEEGLSPSKRRRLSMRNHHSDLT
FCEIILMEMESHDAAWPFLEPVNPRLVSGYRRIIKNPMDFSTMRERLLRGGYTSSEEFAA
DALLVFDNCQTFNEDDSEVGKAGHIMRRFFESRWEEFYQGKQANL
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BDBM50028142 |
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n/a |
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Name | BDBM50028142 |
Synonyms: | CHEMBL2177300 |
Type | Small organic molecule |
Emp. Form. | C25H23ClN2O3 |
Mol. Mass. | 434.915 |
SMILES | C[C@H]1C[C@@H](Nc2ccc(Cl)cc2)c2cc(ccc2N1C(C)=O)-c1ccc(cc1)C(O)=O |r| |
Structure |
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