| Reaction Details |
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 | Report a problem with these data |
| Target | Transcription initiation factor TFIID subunit 1 |
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| Ligand | BDBM26514 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1809384 (CHEMBL4308743) |
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| IC50 | 150±n/a nM |
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| Citation |  Remillard, D; Buckley, DL; Seo, HS; Ferguson, FM; Dhe-Paganon, S; Bradner, JE; Gray, NS Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. ACS Med Chem Lett10:1443-1449 (2019) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Transcription initiation factor TFIID subunit 1 |
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| Name: | Transcription initiation factor TFIID subunit 1 |
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| Synonyms: | BA2R | BA2R | CCG1 | CCGS | Cell cycle gene 1 protein | TAF(II)250 | TAF1 | TAF1_HUMAN | TAF2A | TAFII-250 | TAFII250 | TBP-associated factor 250 kDa | Transcription initiation factor TFIID 250 kDa subunit | Transcription initiation factor TFIID subunit 1 | p250 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 212598.75 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_108248 |
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| Residue: | 1872 |
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| Sequence: | MGPGCDLLLRTAATITAAAIMSDTDSDEDSAGGGPFSLAGFLFGNINGAGQLEGESVLDD
ECKKHLAGLGALGLGSLITELTANEELTGTDGALVNDEGWVRSTEDAVDYSDINEVAEDE
SRRYQQTMGSLQPLCHSDYDEDDYDADCEDIDCKLMPPPPPPPGPMKKDKDQDSITGEKV
DFSSSSDSESEMGPQEATQAESEDGKLTLPLAGIMQHDATKLLPSVTELFPEFRPGKVLR
FLRLFGPGKNVPSVWRSARRKRKKKHRELIQEEQIQEVECSVESEVSQKSLWNYDYAPPP
PPEQCLSDDEITMMAPVESKFSQSTGDIDKVTDTKPRVAEWRYGPARLWYDMLGVPEDGS
GFDYGFKLRKTEHEPVIKSRMIEEFRKLEENNGTDLLADENFLMVTQLHWEDDIIWDGED
VKHKGTKPQRASLAGWLPSSMTRNAMAYNVQQGFAATLDDDKPWYSIFPIDNEDLVYGRW
EDNIIWDAQAMPRLLEPPVLTLDPNDENLILEIPDEKEEATSNSPSKESKKESSLKKSRI
LLGKTGVIKEEPQQNMSQPEVKDPWNLSNDEYYYPKQQGLRGTFGGNIIQHSIPAVELRQ
PFFPTHMGPIKLRQFHRPPLKKYSFGALSQPGPHSVQPLLKHIKKKAKMREQERQASGGG
EMFFMRTPQDLTGKDGDLILAEYSEENGPLMMQVGMATKIKNYYKRKPGKDPGAPDCKYG
ETVYCHTSPFLGSLHPGQLLQAFENNLFRAPIYLHKMPETDFLIIRTRQGYYIRELVDIF
VVGQQCPLFEVPGPNSKRANTHIRDFLQVFIYRLFWKSKDRPRRIRMEDIKKAFPSHSES
SIRKRLKLCADFKRTGMDSNWWVLKSDFRLPTEEEIRAMVSPEQCCAYYSMIAAEQRLKD
AGYGEKSFFAPEEENEEDFQMKIDDEVRTAPWNTTRAFIAAMKGKCLLEVTGVADPTGCG
EGFSYVKIPNKPTQQKDDKEPQPVKKTVTGTDADLRRLSLKNAKQLLRKFGVPEEEIKKL
SRWEVIDVVRTMSTEQARSGEGPMSKFARGSRFSVAEHQERYKEECQRIFDLQNKVLSST
EVLSTDTDSSSAEDSDFEEMGKNIENMLQNKKTSSQLSREREEQERKELQRMLLAAGSAA
SGNNHRDDDTASVTSLNSSATGRCLKIYRTFRDEEGKEYVRCETVRKPAVIDAYVRIRTT
KDEEFIRKFALFDEQHREEMRKERRRIQEQLRRLKRNQEKEKLKGPPEKKPKKMKERPDL
KLKCGACGAIGHMRTNKFCPLYYQTNAPPSNPVAMTEEQEEELEKTVIHNDNEELIKVEG
TKIVLGKQLIESADEVRRKSLVLKFPKQQLPPKKKRRVGTTVHCDYLNRPHKSIHRRRTD
PMVTLSSILESIINDMRDLPNTYPFHTPVNAKVVKDYYKIITRPMDLQTLRENVRKRLYP
SREEFREHLELIVKNSATYNGPKHSLTQISQSMLDLCDEKLKEKEDKLARLEKAINPLLD
DDDQVAFSFILDNIVTQKMMAVPDSWPFHHPVNKKFVPDYYKVIVNPMDLETIRKNISKH
KYQSRESFLDDVNLILANSVKYNGPESQYTKTAQEIVNVCYQTLTEYDEHLTQLEKDICT
AKEAALEEAELESLDPMTPGPYTPQPPDLYDTNTSLSMSRDASVFQDESNMSVLDIPSAT
PEKQVTQEGEDGDGDLADEEEGTVQQPQASVLYEDLLMSEGEDDEEDAGSDEEGDNPFSA
IQLSESGSDSDVGSGGIRPKQPRMLQENTRMDMENEESMMSYEGDGGEASHGLEDSNISY
GSYEEPDPKSNTQDTSFSSIGGYEVSEEEEDEEEEEQRSGPSVLSQVHLSEDEEDSEDFH
SIAGDSDLDSDE
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| BDBM26514 |
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| n/a |
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| Name | BDBM26514 |
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| Synonyms: | 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-N-(1-methylpiperidin-4-yl)benzamide | BI 2536 analogue, 1b |
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| Type | Small organic molecule |
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| Emp. Form. | C27H37N7O2 |
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| Mol. Mass. | 491.6284 |
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| SMILES | CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)C(=O)NC3CCN(C)CC3)ncc2N(C)C1=O |r| |
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| Structure | 
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