Reaction Details Report a problem with these data
Target
Transcription initiation factor TFIID subunit 1
Ligand
BDBM321422
Substrate
n/a
Meas. Tech.
ChEMBL_2300757
IC50
520±n/a nM
Citation
Crawford, TD; Vartanian, S; Côté, A; Bellon, S; Duplessis, M; Flynn, EM; Hewitt, M; Huang, HR; Kiefer, JR; Murray, J; Nasveschuk, CG; Pardo, E; Romero, FA; Sandy, P; Tang, Y; Taylor, AM; Tsui, V; Wang, J; Wang, S; Zawadzke, L; Albrecht, BK; Magnuson, SR; Cochran, AG; Stokoe, D Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance. Bioorg Med Chem Lett 27:3534-3541 (2017) [PubMed]
More Info.:
Target
Name:
Transcription initiation factor TFIID subunit 1
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
Type:
PROTEIN
Mol. Mass.:
212598.75
Organism:
Homo sapiens (Human)
Description:
ChEMBL_108248
Residue:
1872
Sequence:
MGPGCDLLLRTAATITAAAIMSDTDSDEDSAGGGPFSLAGFLFGNINGAGQLEGESVLDDECKKHLAGLGALGLGSLITELTANEELTGTDGALVNDEGWVRSTEDAVDYSDINEVAEDESRRYQQTMGSLQPLCHSDYDEDDYDADCEDIDCKLMPPPPPPPGPMKKDKDQDSITGEKVDFSSSSDSESEMGPQEATQAESEDGKLTLPLAGIMQHDATKLLPSVTELFPEFRPGKVLRFLRLFGPGKNVPSVWRSARRKRKKKHRELIQEEQIQEVECSVESEVSQKSLWNYDYAPPPPPEQCLSDDEITMMAPVESKFSQSTGDIDKVTDTKPRVAEWRYGPARLWYDMLGVPEDGSGFDYGFKLRKTEHEPVIKSRMIEEFRKLEENNGTDLLADENFLMVTQLHWEDDIIWDGEDVKHKGTKPQRASLAGWLPSSMTRNAMAYNVQQGFAATLDDDKPWYSIFPIDNEDLVYGRWEDNIIWDAQAMPRLLEPPVLTLDPNDENLILEIPDEKEEATSNSPSKESKKESSLKKSRILLGKTGVIKEEPQQNMSQPEVKDPWNLSNDEYYYPKQQGLRGTFGGNIIQHSIPAVELRQPFFPTHMGPIKLRQFHRPPLKKYSFGALSQPGPHSVQPLLKHIKKKAKMREQERQASGGGEMFFMRTPQDLTGKDGDLILAEYSEENGPLMMQVGMATKIKNYYKRKPGKDPGAPDCKYGETVYCHTSPFLGSLHPGQLLQAFENNLFRAPIYLHKMPETDFLIIRTRQGYYIRELVDIFVVGQQCPLFEVPGPNSKRANTHIRDFLQVFIYRLFWKSKDRPRRIRMEDIKKAFPSHSESSIRKRLKLCADFKRTGMDSNWWVLKSDFRLPTEEEIRAMVSPEQCCAYYSMIAAEQRLKDAGYGEKSFFAPEEENEEDFQMKIDDEVRTAPWNTTRAFIAAMKGKCLLEVTGVADPTGCGEGFSYVKIPNKPTQQKDDKEPQPVKKTVTGTDADLRRLSLKNAKQLLRKFGVPEEEIKKLSRWEVIDVVRTMSTEQARSGEGPMSKFARGSRFSVAEHQERYKEECQRIFDLQNKVLSSTEVLSTDTDSSSAEDSDFEEMGKNIENMLQNKKTSSQLSREREEQERKELQRMLLAAGSAASGNNHRDDDTASVTSLNSSATGRCLKIYRTFRDEEGKEYVRCETVRKPAVIDAYVRIRTTKDEEFIRKFALFDEQHREEMRKERRRIQEQLRRLKRNQEKEKLKGPPEKKPKKMKERPDLKLKCGACGAIGHMRTNKFCPLYYQTNAPPSNPVAMTEEQEEELEKTVIHNDNEELIKVEGTKIVLGKQLIESADEVRRKSLVLKFPKQQLPPKKKRRVGTTVHCDYLNRPHKSIHRRRTDPMVTLSSILESIINDMRDLPNTYPFHTPVNAKVVKDYYKIITRPMDLQTLRENVRKRLYPSREEFREHLELIVKNSATYNGPKHSLTQISQSMLDLCDEKLKEKEDKLARLEKAINPLLDDDDQVAFSFILDNIVTQKMMAVPDSWPFHHPVNKKFVPDYYKVIVNPMDLETIRKNISKHKYQSRESFLDDVNLILANSVKYNGPESQYTKTAQEIVNVCYQTLTEYDEHLTQLEKDICTAKEAALEEAELESLDPMTPGPYTPQPPDLYDTNTSLSMSRDASVFQDESNMSVLDIPSATPEKQVTQEGEDGDGDLADEEEGTVQQPQASVLYEDLLMSEGEDDEEDAGSDEEGDNPFSAIQLSESGSDSDVGSGGIRPKQPRMLQENTRMDMENEESMMSYEGDGGEASHGLEDSNISYGSYEEPDPKSNTQDTSFSSIGGYEVSEEEEDEEEEEQRSGPSVLSQVHLSEDEEDSEDFHSIAGDSDLDSDE
Inhibitor
Name:
BDBM321422
Synonyms:
5-[6-[(E)-but-2-enyl]-2-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]-2-(morpholine-4-carbonyl)benzonitrile | US10183009, Example 106
Type:
Small organic molecule
Emp. Form.:
C24H24N4O3
Mol. Mass.:
416.4724
SMILES:
C\C=C\Cn1cc(-c2ccc(C(=O)N3CCOCC3)c(c2)C#N)c2cc(C)[nH]c2c1=O