Ki Summary

Reaction Details

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Target

Histone acetyltransferase p300

Ligand

BDBM50255527

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_515393 (CHEMBL1025548)

IC50

6620±n/a nM

Citation

Wu, J; Xie, N; Wu, Z; Zhang, Y; Zheng, YG Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60. Bioorg Med Chem17:1381-6 (2009) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Histone acetyltransferase p300

Name:

Histone acetyltransferase p300

Synonyms:

EP300 | EP300_HUMAN | HIF1A/p300/CREB-binding protein | Histone acetyltransferase p300/Hypoxia-inducible factor 1-alpha | P300

Type:

Protein

Mol. Mass.:

264223.04

Organism:

Homo sapiens (Human)

Description:

Q09472

Residue:

2414

Sequence:

MAENVVEPGPPSAKRPKLSSPALSASASDGTDFGSLFDLEHDLPDELINSTELGLTNGGD
INQLQTSLGMVQDAASKHKQLSELLRSGSSPNLNMGVGGPGQVMASQAQQSSPGLGLINS
MVKSPMTQAGLTSPNMGMGTSGPNQGPTQSTGMMNSPVNQPAMGMNTGMNAGMNPGMLAA
GNGQGIMPNQVMNGSIGAGRGRQNMQYPNPGMGSAGNLLTEPLQQGSPQMGGQTGLRGPQ
PLKMGMMNNPNPYGSPYTQNPGQQIGASGLGLQIQTKTVLSNNLSPFAMDKKAVPGGGMP
NMGQQPAPQVQQPGLVTPVAQGMGSGAHTADPEKRKLIQQQLVLLLHAHKCQRREQANGE
VRQCNLPHCRTMKNVLNHMTHCQSGKSCQVAHCASSRQIISHWKNCTRHDCPVCLPLKNA
GDKRNQQPILTGAPVGLGNPSSLGVGQQSAPNLSTVSQIDPSSIERAYAALGLPYQVNQM
PTQPQVQAKNQQNQQPGQSPQGMRPMSNMSASPMGVNGGVGVQTPSLLSDSMLHSAINSQ
NPMMSENASVPSLGPMPTAAQPSTTGIRKQWHEDITQDLRNHLVHKLVQAIFPTPDPAAL
KDRRMENLVAYARKVEGDMYESANNRAEYYHLLAEKIYKIQKELEEKRRTRLQKQNMLPN
AAGMVPVSMNPGPNMGQPQPGMTSNGPLPDPSMIRGSVPNQMMPRITPQSGLNQFGQMSM
AQPPIVPRQTPPLQHHGQLAQPGALNPPMGYGPRMQQPSNQGQFLPQTQFPSQGMNVTNI
PLAPSSGQAPVSQAQMSSSSCPVNSPIMPPGSQGSHIHCPQLPQPALHQNSPSPVPSRTP
TPHHTPPSIGAQQPPATTIPAPVPTPPAMPPGPQSQALHPPPRQTPTPPTTQLPQQVQPS
LPAAPSADQPQQQPRSQQSTAASVPTPTAPLLPPQPATPLSQPAVSIEGQVSNPPSTSST
EVNSQAIAEKQPSQEVKMEAKMEVDQPEPADTQPEDISESKVEDCKMESTETEERSTELK
TEIKEEEDQPSTSATQSSPAPGQSKKKIFKPEELRQALMPTLEALYRQDPESLPFRQPVD
PQLLGIPDYFDIVKSPMDLSTIKRKLDTGQYQEPWQYVDDIWLMFNNAWLYNRKTSRVYK
YCSKLSEVFEQEIDPVMQSLGYCCGRKLEFSPQTLCCYGKQLCTIPRDATYYSYQNRYHF
CEKCFNEIQGESVSLGDDPSQPQTTINKEQFSKRKNDTLDPELFVECTECGRKMHQICVL
HHEIIWPAGFVCDGCLKKSARTRKENKFSAKRLPSTRLGTFLENRVNDFLRRQNHPESGE
VTVRVVHASDKTVEVKPGMKARFVDSGEMAESFPYRTKALFAFEEIDGVDLCFFGMHVQE
YGSDCPPPNQRRVYISYLDSVHFFRPKCLRTAVYHEILIGYLEYVKKLGYTTGHIWACPP
SEGDDYIFHCHPPDQKIPKPKRLQEWYKKMLDKAVSERIVHDYKDIFKQATEDRLTSAKE
LPYFEGDFWPNVLEESIKELEQEEEERKREENTSNESTDVTKGDSKNAKKKNNKKTSKNK
SSLSRGNKKKPGMPNVSNDLSQKLYATMEKHKEVFFVIRLIAGPAANSLPPIVDPDPLIP
CDLMDGRDAFLTLARDKHLEFSSLRRAQWSTMCMLVELHTQSQDRFVYTCNECKHHVETR
WHCTVCEDYDLCITCYNTKNHDHKMEKLGLGLDDESNNQQAAATQSPGDSRRLSIQRCIQ
SLVHACQCRNANCSLPSCQKMKRVVQHTKGCKRKTNGGCPICKQLIALCCYHAKHCQENK
CPVPFCLNIKQKLRQQQLQHRLQQAQMLRRRMASMQRTGVVGQQQGLPSPTPATPTTPTG
QQPTTPQTPQPTSQPQPTPPNSMPPYLPRTQAAGPVSQGKAAGQVTPPTPPQTAQPPLPG
PPPAAVEMAMQIQRAAETQRQMAHVQIFQRPIQHQMPPMTPMAPMGMNPPPMTRGPSGHL
EPGMGPTGMQQQPPWSQGGLPQPQQLQSGMPRPAMMSVAQHGQPLNMAPQPGLGQVGISP
LKPGTVSQQALQNLLRTLRSPSSPLQQQQVLSILHANPQLLAAFIKQRAAKYANSNPQPI
PGQPGMPQGQPGLQPPTMPGQQGVHSNPAMQNMNPMQAGVQRAGLPQQQPQQQLQPPMGG
MSPQAQQMNMNHNTMPSQFRDILRRQQMMQQQQQQGAGPGIGPGMANHNQFQQPQGVGYP
PQQQQRMQHHMQQMQQGNMGQIGQLPQALGAEAGASLQAYQQRLLQQQMGSPVQPNPMSP
QQHMLPNQAQSPHLQGQQIPNSLSNQVRSPQPVPSPRPQSQPPHSSPSPRMQPQPSPHHV
SPQTSSPHPGLVAAQANPMEQGHFASPDQNSMLSQLASNPGMANLHGASATDLGLSTDNS
DLNSNLSQSTLDIH

BDBM50255527

n/a

Name

BDBM50255527

Synonyms:

Ac-SGRGKGGKGLGKGGAK(CoA)RHRK | CHEMBL504265

Type

Small organic molecule

Emp. Form.

C107H188N43O40P3S

Mol. Mass.

2841.888

SMILES

CC(C)C[C@H](NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)CNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)CSCCNC(=O)CCNC(=O)[C@H](O)C(C)(C)COP(O)(=O)OP(O)(=O)OC[C@H]1O[C@H]([C@H](O)[C@@H]1OP(O)(O)=O)n1cnc2c(N)ncnc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(O)=O |r,wU:134.135,88.88,132.132,42.49,29.34,153.155,113.113,57.59,174.177,wD:129.128,131.140,4.4,71.70,93.92,164.166,185.188,12.17,(30.67,-41.69,;30.67,-40.13,;32,-39.37,;29.35,-39.36,;29.36,-37.8,;28.03,-37.02,;26.75,-37.88,;26.74,-39.43,;25.41,-37.1,;24.02,-37.78,;22.68,-37.02,;22.69,-35.49,;21.33,-37.79,;21.32,-39.35,;22.65,-40.11,;22.64,-41.67,;23.97,-42.44,;23.87,-43.9,;20,-37.02,;18.66,-37.79,;18.66,-39.32,;17.32,-37,;15.97,-37.76,;14.64,-36.99,;14.63,-35.44,;13.31,-37.76,;11.98,-36.98,;10.65,-37.76,;10.64,-39.29,;9.31,-36.98,;9.31,-35.43,;10.66,-34.65,;10.66,-33.13,;12.01,-32.35,;12.01,-30.76,;7.94,-37.69,;6.59,-36.95,;6.59,-35.4,;5.26,-37.71,;3.95,-36.9,;2.66,-37.74,;2.66,-39.27,;1.32,-36.95,;1.32,-35.4,;2.67,-34.63,;2.67,-33.09,;3.94,-32.22,;4.02,-30.68,;2.63,-29.8,;5.31,-29.81,;-.07,-37.62,;-1.43,-36.91,;-1.43,-35.35,;-2.75,-37.67,;-4.05,-36.84,;-5.31,-37.74,;-5.31,-39.27,;-6.66,-36.95,;-6.64,-35.4,;-5.3,-34.63,;-8,-37.7,;-9.34,-36.95,;-10.66,-37.71,;-9.34,-35.39,;30.68,-37.05,;30.69,-35.52,;32.02,-37.81,;33.39,-37.13,;34.73,-37.91,;34.73,-39.46,;36.02,-37.07,;37.34,-37.87,;37.35,-39.42,;38.66,-40.19,;38.66,-41.74,;39.98,-42.51,;39.91,-44,;38.67,-37.1,;38.68,-35.57,;40.01,-37.86,;41.39,-37.16,;42.72,-37.94,;42.72,-39.5,;44.02,-37.11,;45.34,-37.9,;46.66,-37.14,;46.67,-35.61,;48.01,-37.89,;49.38,-37.18,;49.38,-35.65,;50.72,-37.96,;50.71,-39.51,;52.02,-37.14,;53.34,-37.93,;53.34,-39.48,;54.66,-40.25,;54.66,-41.8,;55.98,-42.57,;55.92,-44.11,;54.6,-44.91,;54.59,-46.45,;53.26,-44.13,;51.92,-44.9,;51.91,-46.43,;50.57,-47.2,;50.52,-48.74,;51.86,-49.52,;53.19,-48.75,;51.85,-51.07,;53.18,-51.84,;53.15,-53.38,;51.81,-54.15,;50.47,-53.37,;51.8,-55.68,;50.42,-56.44,;53.13,-56.45,;54.47,-57.22,;52.35,-57.79,;53.9,-55.13,;55.45,-55.13,;56.22,-53.81,;56.91,-52.5,;54.89,-53.04,;57.56,-54.59,;58.89,-53.83,;60.17,-53.04,;58.13,-52.49,;59.67,-55.17,;58.89,-56.51,;59.65,-57.84,;59,-59.26,;60.14,-60.28,;61.48,-59.53,;62.78,-60.2,;61.17,-58.02,;62.22,-56.89,;63.72,-57.22,;65.15,-57.57,;64,-55.71,;63.38,-58.73,;59.97,-61.82,;58.64,-62.58,;58.95,-64.09,;60.47,-64.26,;61.37,-65.51,;60.73,-66.91,;62.91,-65.37,;63.54,-63.97,;62.64,-62.71,;61.11,-62.86,;54.67,-37.17,;54.68,-35.63,;56.01,-37.93,;57.37,-37.2,;57.37,-35.67,;58.72,-34.9,;58.73,-33.37,;60.05,-32.57,;60.08,-31.03,;58.72,-30.23,;61.38,-30.24,;58.7,-37.98,;58.7,-39.54,;60.02,-37.18,;61.34,-37.97,;61.33,-39.52,;62.65,-40.29,;64.03,-39.7,;65.07,-40.84,;64.3,-42.17,;62.8,-41.83,;62.66,-37.21,;62.66,-35.68,;64,-37.97,;65.34,-37.21,;65.34,-35.69,;66.69,-34.92,;66.7,-33.39,;68.04,-32.63,;68.07,-31.09,;66.7,-30.33,;69.4,-30.32,;66.68,-38,;66.68,-39.55,;68.01,-37.23,;69.34,-38,;69.34,-39.56,;70.67,-40.32,;70.67,-41.88,;71.98,-42.65,;71.98,-44.2,;70.67,-37.24,;72.02,-38.02,;70.69,-35.71,)|

Structure