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nprot.2014.138#supplementary-information
115. Philpott M, Yang J, Tumber T, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Keates T,
Felletar I, Ciulli A, Knapp S, Heightman TD (2011) Bromodomain-peptide displacement
assays for interactome mapping and inhibitor discovery. Mol BioSyst 7(10):2899–2908.
https://doi.org/10.1039/c1mb05099k
116. Roberts JM, Bradner JE (2015) A bead-based proximity assay for BRD4 ligand discovery.
Curr Protoc Chem Biol 7(4):263–278. https://doi.org/10.1002/9780470559277.ch150024
117. Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M,
Martin SJ, Felletar I, Marsden BD, Filippakopoulos P, Muller S, Knapp S, Brennan PE (2014)
[1,2,4]Triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. J Med Chem
57(2):462–476. https://doi.org/10.1021/jm401568s
118. Ciceri P, Mueller S, O’Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA,
Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S (2014)
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem
Biol 10(4):305–312. https://doi.org/10.1038/nchembio.1471
119. Crawford TD, Audia JE, Bellon S, Burdick DJ, Bommi-Reddy A, Cote A, Cummings RT,
Duplessis M, Flynn EM, Hewitt M, Huang H-R, Jayaram H, Jiang Y, Joshi S, Kiefer JR,
Murray J, Nasveschuk CG, Neiss A, Pardo E, Romero FA, Sandy P, Sims RJ, Tang Y, Taylor
AM, Tsui V, Wang J, Wang S, Wang Y, Xu Z, Zawadzke L, Zhu X, Albrecht BK, Magnuson
SR, Cochran AG (2017) GNE-886: a potent and selective inhibitor of the cat eye syndrome
chromosome region candidate 2 bromodomain (CECR2). ACS Med Chem Lett 8(7):737–741.
https://doi.org/10.1021/acsmedchemlett.7b00132
120. Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung C-w, Fedorov O,
Grandi P, Jung D, Lesniak R, Lindon M, Muller S, Philpott M, Prinjha R, Rogers C,
Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH (2016) Discovery and
characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and
BAZ2B. J Med Chem 59(4):1410–1424. https://doi.org/10.1021/acs.jmedchem.5b00209
121. Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL,
Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE,
Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR, Cote A, Jayaram H,
Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy F, Spillane KL, Wang F,
Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X, Bellon S, Cummings R, Cochran AG,
Albrecht BK, Magnuson S (2016) Discovery of a potent and selective in vivo probe
(GNE-272) for the bromodomains of CBP/EP300. J Med Chem 59(23):10549–10563.
https://doi.org/10.1021/acs.jmedchem.6b01022
122. Humphreys PG, Bamborough P, Chung C-w, Craggs PD, Gordon L, Grandi P, Hayhow TG,
Hussain J, Jones KL, Lindon M, Michon A-M, Renaux JF, Suckling CJ, Tough DF, Prinjha
RK (2017) Discovery of a potent, cell penetrant, and selective p300/CBP-associated factor
(PCAF)/general control nonderepressible 5 (GCN5) bromodomain chemical probe. J Med
Chem 60(2):695–709. https://doi.org/10.1021/acs.jmedchem.6b01566
123. Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung C-w,
Dittmann A, Drewes G, Drewry DH, Gordon L, Grandi P, Leveridge M, Lindon M, Michon
A-M, Molnar J, Robson SC, Tomkinson NCO, Kouzarides T, Prinjha RK, Humphreys PG
(2016) Discovery of I-BRD9, a selective cell active chemical probe for bromodomain
containing protein 9 inhibition. J Med Chem 59(4):1425–1439. https://doi.org/10.1021/acs.
jmedchem.5b00256
124. Kenakin TP (1993) Pharmacological analysis of drug-receptor interaction. Raven, New York
125. Chung C-W, Coste H, White JH, Mirguet O, Wilde J, Gosmini RL, Delves C, Magny SM,
Woodward R, Hughes SA, Boursier EV, Flynn H, Bouillot AM, Bamborough P, Brusq J-MG,
Gellibert FJ, Jones EJ, Riou AM, Homes P, Martin SL, Uings IJ, Toum J, Clément CA,
Applied Biophysics for Bromodomain Drug Discovery
335