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Crystal structure of WDR5 in complex with MYC MbIIIb peptide
Descriptor:	1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, MYC MbIIIb peptide, ...
Authors:	Sun, Q, Phan, J, Olejniczak, E.T, Thomas, L.R, Fesik, S.W, Tansey, W.P.
Deposit date:	2015-02-16
Release date:	2015-04-15
Last modified:	2023-09-27
Method:	X-RAY DIFFRACTION (1.898 Å)
Cite:	Interaction with WDR5 Promotes Target Gene Recognition and Tumorigenesis by MYC. Mol.Cell, 58, 2015

3CLP

M. loti cyclic-nucleotide binding domain mutant 2
Descriptor:	ADENOSINE-3',5'-CYCLIC-MONOPHOSPHATE, Mll3241 protein
Authors:	Clayton, G.M, Altieri, S.L, Thomas, L.R, Morais-Cabral, J.H.
Deposit date:	2008-03-19
Release date:	2008-08-05
Last modified:	2024-02-21
Method:	X-RAY DIFFRACTION (2 Å)
Cite:	Structural and Energetic Analysis of Activation by a Cyclic Nucleotide Binding Domain. J.Mol.Biol., 381, 2008

3CO2

Mlotik1 ion channel cyclic-nucleotide binding domain mutant
Descriptor:	Mlotik1 ion channel protein
Authors:	Clayton, G.M, Alteiri, S.L, Thomas, L.R, Morais-Cabral, J.H.
Deposit date:	2008-03-27
Release date:	2008-08-05
Last modified:	2024-02-21
Method:	X-RAY DIFFRACTION (2.9 Å)
Cite:	Structural and Energetic Analysis of Activation by a Cyclic Nucleotide Binding Domain. J.Mol.Biol., 381, 2008

3CL1

M. loti cyclic-nucleotide binding domain, cyclic-GMP bound
Descriptor:	CHLORIDE ION, CYCLIC GUANOSINE MONOPHOSPHATE, Mll3241 protein, ...
Authors:	Clayton, G.M, Alteiri, S.L, Thomas, L.R, Morais-Cabral, J.H.
Deposit date:	2008-03-18
Release date:	2008-08-05
Last modified:	2024-02-21
Method:	X-RAY DIFFRACTION (2.4 Å)
Cite:	Structural and Energetic Analysis of Activation by a Cyclic Nucleotide Binding Domain. J.Mol.Biol., 381, 2008

6DY7

WDR5 in complex with a WIN site inhibitor
Descriptor:	DIMETHYL SULFOXIDE, N-[3-(2,4-dichlorophenoxy)propyl]-1H-imidazol-2-amine, SULFATE ION, ...
Authors:	Phan, J, Wang, F, Fesik, S.W.
Deposit date:	2018-07-01
Release date:	2019-03-13
Last modified:	2024-03-13
Method:	X-RAY DIFFRACTION (1.9 Å)
Cite:	Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep, 26, 2019

6E1Y

Discovery of Potent 2-Aryl-6,7-Dihydro-5HPyrrolo[ 1,2-a]imidazoles as WDR5 WIN-site Inhibitors Using Fragment-Based Methods and Structure-Based Design
Descriptor:	N-[(1S)-1-(3-chlorophenyl)ethyl]-3-{[(4,5-dihydro-1H-imidazol-2-yl)amino]methyl}benzamide, WD repeat-containing protein 5
Authors:	Phan, J, Fesik, S.W.
Deposit date:	2018-07-10
Release date:	2019-03-13
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.219 Å)
Cite:	Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep, 26, 2019

6DYA

WDR5 in complex with a WIN site inhibitor
Descriptor:	DIMETHYL SULFOXIDE, N-[(3,5-dichlorophenyl)methyl]-3-[(1H-imidazol-1-yl)methyl]benzamide, SULFATE ION, ...
Authors:	Phan, J, Wang, F, Fesik, S.W.
Deposit date:	2018-07-01
Release date:	2019-03-13
Last modified:	2024-03-13
Method:	X-RAY DIFFRACTION (2.56 Å)
Cite:	Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep, 26, 2019

6E1Z

Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
Descriptor:	5-[(1H-imidazol-1-yl)methyl]furan-2-carboxylic acid, WD repeat-containing protein 5
Authors:	Phan, J, Fesik, S.W.
Deposit date:	2018-07-10
Release date:	2019-03-13
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.1 Å)
Cite:	Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep, 26, 2019

6E23

Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
Descriptor:	4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, N-[(3,4-dichlorophenyl)methyl]-3-(6-fluoro-2-methylpyridin-3-yl)-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}benzamide, WD repeat-containing protein 5
Authors:	Phan, J, Fesik, S.W.
Deposit date:	2018-07-10
Release date:	2019-03-13
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.66 Å)
Cite:	Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep, 26, 2019

6E22

Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
Descriptor:	3-{[(4,5-dihydro-1H-imidazol-2-yl)amino]methyl}-N-[(3,5-dimethoxyphenyl)methyl]-4-fluorobenzamide, SULFATE ION, WD repeat-containing protein 5
Authors:	Phan, J, Fesik, S.W.
Deposit date:	2018-07-10
Release date:	2019-03-13
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.6 Å)
Cite:	Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep, 26, 2019

6U80

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction
Descriptor:	5-bromo-N-(4-hydroxy[1,1'-biphenyl]-3-yl)-2-methoxybenzene-1-sulfonamide, WD repeat-containing protein 5
Authors:	Zhao, B, Wang, F.
Deposit date:	2019-09-04
Release date:	2019-12-04
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.55 Å)
Cite:	Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J.Med.Chem., 62, 2019

6UFX

WD repeat-containing protein 5 complexed with N-[(3,5-dimethoxyphenyl)methyl]-4'-fluoro-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}-2'-methyl[1,1'-biphenyl]-3-carboxamide (compound 13)
Descriptor:	N-[(3,5-dimethoxyphenyl)methyl]-4'-fluoro-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}-2'-methyl[1,1'-biphenyl]-3-carboxamide, WD repeat-containing protein 5
Authors:	Rietz, T.A, Fesik, S.W, Zhao, B.
Deposit date:	2019-09-25
Release date:	2020-01-01
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (2.015 Å)
Cite:	Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core. J.Med.Chem., 63, 2020

6UCS

Discovery and Structure-Based optimization of potent and selective WDR5 inhibitors containing a dihydroisoquinolinone bicyclic core
Descriptor:	7-[(2-azanyl-3-methyl-imidazol-1-yl)methyl]-2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoranyl-2-methyl-phenyl)-3,4-dihydroisoquinolin-1-one, WD repeat-containing protein 5
Authors:	Zhao, B.
Deposit date:	2019-09-17
Release date:	2020-01-01
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.85 Å)
Cite:	Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core. J.Med.Chem., 63, 2020

6UIF

Discovery of fragment-inspired heterocyclic benzenesulfonmides as inhibitors of the WDR5-MYC interaction
Descriptor:	4-{[(5-bromo-3-chloro-2-hydroxyphenyl)sulfonyl]amino}-1-cyclopentyl-N-methyl-1H-imidazole-2-carboxamide, WD repeat domain 5
Authors:	Zhao, B.
Deposit date:	2019-09-30
Release date:	2020-04-15
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.603 Å)
Cite:	Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J.Med.Chem., 63, 2020

6U5Y

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction
Descriptor:	3-{[(5-bromo-3-chloro-2-hydroxyphenyl)sulfonyl]amino}-5-(1-cyanocyclobutyl)-2-hydroxy-N-methylbenzamide, WD repeat-containing protein 5
Authors:	Zhao, B, Wang, F.
Deposit date:	2019-08-28
Release date:	2019-12-04
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.532 Å)
Cite:	Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J.Med.Chem., 62, 2019

6UIK

Discovery of fragment-inspired heterocyclic benzenesulfonmides as inhibitors of the WDR5-MYC interaction
Descriptor:	5-bromo-3-chloro-N-(1-cyclopentyl-1H-imidazol-4-yl)-2-hydroxybenzene-1-sulfonamide, WD repeat domanin 5
Authors:	Zhao, B.
Deposit date:	2019-10-01
Release date:	2020-04-15
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.6 Å)
Cite:	Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J.Med.Chem., 63, 2020

6U5M

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction
Descriptor:	5-bromo-2-hydroxy-N-[3-(methylsulfonyl)-5-(pentafluoro-lambda~6~-sulfanyl)phenyl]benzene-1-sulfonamide, WD repeat-containing protein 5
Authors:	Zhao, B, Wang, F.
Deposit date:	2019-08-28
Release date:	2019-12-04
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.8 Å)
Cite:	Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J.Med.Chem., 62, 2019

6U8B

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction
Descriptor:	3-{[(5-bromo-2-methoxyphenyl)sulfonyl]amino}-5-chloro-2-hydroxybenzoic acid, WD repeat-containing protein 5
Authors:	Zhao, B, Wang, F.
Deposit date:	2019-09-04
Release date:	2019-12-04
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.261 Å)
Cite:	Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J.Med.Chem., 62, 2019

6UJH

Discovery of fragment-inspired heterocyclic benzenesulfonamides as inhibitors of the WDR5-MYC interaction
Descriptor:	(2R)-2-(4-chlorophenyl)-3-oxobutanenitrile, DIMETHYL SULFOXIDE, SULFATE ION, ...
Authors:	Phan, J, Fesik, S.W.
Deposit date:	2019-10-03
Release date:	2020-04-15
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.493 Å)
Cite:	Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J.Med.Chem., 63, 2020

6U6W

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction
Descriptor:	5-bromo-N-(5-chloro-2-hydroxyphenyl)-2-methoxybenzene-1-sulfonamide, WD repeat-containing protein 5
Authors:	Zhao, B, Wang, F.
Deposit date:	2019-08-30
Release date:	2019-12-04
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.2 Å)
Cite:	Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J.Med.Chem., 62, 2019

6UJ4

Discovery of fragment-inspired heterocyclic benzenesulfonmides as inhibitors of the WDR5-MYC interaction
Descriptor:	5-bromo-3-chloro-N-(1-cyclopentyl-2-methyl-1H-imidazol-4-yl)-2-hydroxybenzene-1-sulfonamide, WD repeat domain 5
Authors:	Zhao, B.
Deposit date:	2019-10-02
Release date:	2020-04-15
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.53 Å)
Cite:	Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J.Med.Chem., 63, 2020

6UJL

Discovery of fragment-inspired heterocyclic benzenesulfonamides as inhibitors of the WDR5-MYC interaction
Descriptor:	6-methyl-3-(propylsulfanyl)-1,2,4-triazin-5-ol, WD repeat-containing protein 5
Authors:	Phan, J.
Deposit date:	2019-10-03
Release date:	2020-04-15
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.599 Å)
Cite:	Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J.Med.Chem., 63, 2020

6U8O

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction
Descriptor:	5-bromo-N-[5-(1-cyanocyclobutyl)-2-hydroxyphenyl]-2-hydroxybenzene-1-sulfonamide, WD repeat-containing protein 5
Authors:	Zhao, B, Wang, F.
Deposit date:	2019-09-05
Release date:	2019-12-04
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.6 Å)
Cite:	Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J.Med.Chem., 62, 2019

6U8L

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction
Descriptor:	3-{[(5-bromo-2-hydroxyphenyl)sulfonyl]amino}-5-cyclopropyl-6-fluoro-2-hydroxybenzoic acid, N-[2-(4-methylpiperazin-1-yl)-5-nitrophenyl]isoquinolin-1-amine, WD repeat-containing protein 5
Authors:	Zhao, B, Wang, F.
Deposit date:	2019-09-05
Release date:	2019-12-04
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.57 Å)
Cite:	Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J.Med.Chem., 62, 2019

6UJJ

Discovery of fragment-inspired heterocyclic benzenesulfonamides as inhibitors of the WDR5-MYC interaction
Descriptor:	5-[4-(trifluoromethyl)phenyl]-1H-tetrazole, WD repeat-containing protein 5
Authors:	Phan, J.
Deposit date:	2019-10-03
Release date:	2020-04-15
Last modified:	2023-10-11
Method:	X-RAY DIFFRACTION (1.731 Å)
Cite:	Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J.Med.Chem., 63, 2020

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