The Ligandable Human Proteome

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Heat shock protein HSP 90-alpha

Histidine kinase/HSP90-like ATPase

IndexLigand NameStructurePDB codeCompound Potency nM
19unStructure of HSP90 with NMS-E973 inhibitor bound4b7p0.346
2whaHsp90 alpha N-terminal domain in complex with a tricyclic inhibitor3wha0.48
3vheHsp90 alpha N-terminal domain in complex with a macrocyclic inhibitor, CH51648403vhd0.52
4vhdStructure of HSP90 with an inhibitor bound2xab0.54
5xjxStructure of HSP90 with small molecule inhibitor bound2xjx0.71
61rcHSP90 N-terminal domain in complex with (1R)-2-(5-chloro-2,4-dihydroxybenzoyl)-N-ethylisoindoline-1-carboxamide3k981
7vhcHsp90 alpha N-terminal domain in complex with a macrocyclic inhibitor3vhc1.3
894mHSP90A N-terminal domain in complex with BIIB0213qdd1.7
92lcCorrelation between chemotype-dependent binding conformations of HSP90 alpha/beta and isoform selectivity4nh83
10e0gCorrelation between chemotype-dependent binding conformations of HSP90 alpha/beta and isoform selectivity4nh74
112ggInhibition of the HSP90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole, isoxazole amide analogs2uwd4.5
12c0pStructure of HSP90 with small molecule inhibitor bound2xhr4.8
132qaIdentification of novel HSP90/isoform selective inhibitors using structure-based drug design. Demonstration of potential utility in treating CNS disorders such as Huntington's disease4o0b5
14hajHuman HSP90 alpha N-terminal domain in complex with an Aminotriazoloquinazoline inhibitor4cwr5
15bd0HSP90 N-terminal domain in complex with 1-{4-[(2R)-1-(5-chloro-2,4-dihydroxybenzoyl)pyrrolidin-2-yl]benzyl}-3,3-difluoropyrrolidinium3hek5.4
16fu3Optimization of Potent, Selective, and Orally Bioavailable Pyrrolodinopyrimidine-containing Inhibitors of Heat Shock Protein 90. Identification of Development Candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide3r4o7
174cdHSP90 N-terminal domain in complex with 4-chloro-6-{[(2R)-2-(2-methylphenyl)pyrrolidin-1-yl]carbonyl}benzene-1,3-diol3k9710
18fu7Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide3r4p11
19g3rHuman HSP90 alpha N-terminal domain in complex with an Aminotriazoloquinazoline inhibitor4cws12
20990Crystal Structure of Hsp90-alpha N-domain Bound to the Inhibitor NVP-HSP9904u9313
21xjgStructure of HSP90 with small molecule inhibitor bound2xjg15
22rdcHuman Hsp90-alpha ATPase domain bound to Radicicol4egk19
23bsmCrystal Structure of HSP90 with VER-490093owb19
242r6Identification of novel HSP90 / isoform selective inhibitors using structure-based drug design. Demonstration of potential utility in treating CNS disorders such as Huntington s disease4o0920
252gj4,5 Diaryl Isoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer2vci21
262eq4,5 Diaryl Isoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer2vcj21
27fj6Crystal Structure of the human Hsp90-alpha N-domain bound to the hsp90 inhibitor FJ64lwi23
2899bComplex of HSP90 ATPase domain with tropane derived inhibitors4awo24
29fj5Crystal Structure of the human Hsp90-alpha N-domain bound to the hsp90 inhibitor FJ54lwh27
30cxzDiscovery of Benzisoxazoles as Potent Inhibitors of Chaperone Hsp903bmy30
31py9Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone3ekr30
32mojStructure of HSP90 bound with a noval fragment.3ft830
332q9Identification of novel HSP90/isoform selective inhibitors using structure-based drug design. Demonstration of potential utility in treating CNS disorders such as Huntington's disease4o0537
34vhaHsp90 alpha N-terminal domain in complex with a macrocyclic inhibitor3vha40
35819Human heat-shock protein 90 (HSP90) in complex with {4-[3-(2,4-dihydroxy-5-isopropyl-phenyl)-5-thioxo- 1,5-dihydro-[1,2,4]triazol-4-yl]-benzyl}-carbamic acid ethyl ester {ZK 2819}3hhu41
36fghIdentification of novel HSP90/isoform selective inhibitors using structure-based drug design. Demonstration of potential utility in treating CNS disorders such as Huntington's disease4o0742
37h71Structure of human Hsp90-alpha bound to the potent water soluble inhibitor PU-H712fwz50
3840zDiscovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors4xit54
392klOrally Active 2-Amino Thienopyrimidine Inhibitors of the Hsp90 Chaperone2wi758
40pftHSP90 N-terminal domain in complex with 4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)benzene-1,3-diol3k9960
41fj2Crystal Structure of the human Hsp90-alpha N-domain bound to the hsp90 inhibitor FJ24lwe70
4299aComplex of HSP90 ATPase domain with tropane derived inhibitors4awp81
4306tDiscovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.3rkz83
4440yDiscovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors4xiq86
4506hMacrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity.3r9192
4605sDesign and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity3qtf110
4740xDiscovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors4xir115
48fu5Optimization of Potent, Selective, and Orally Bioavailable Pyrrolodinopyrimidine-containing Inhibitors of Heat Shock Protein 90. Identification of Development Candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide3r4n130
49tv2Human HSP90 alpha N-terminal domain in complex with an Aminotriazoloquinazoline inhibitor4cwp170
50ik9Human HSP90 alpha N-terminal domain in complex with an Aminotriazoloquinazoline inhibitor4cwt179
51h64Structure of human Hsp90-alpha bound to the potent water soluble inhibitor PU-H642fwy200
52zz6Orally Active 2-Amino Thienopyrimidine Inhibitors of the Hsp90 Chaperone2wi6230
5340wDiscovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors4xip235
54t5mStructure of HSP90 with small molecule inhibitor bound2xhx250
55efuHsp90 Alpha N-terminal Domain in Complex with an Inhibitor 6-Hydroxy-3-(3-methyl-benzyl)-1H-indazole-5-carboxylic acid benzyl-methyl-amide4efu250
562d73-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as Inhibitors of the Hsp90 Molecular Chaperone2byh258
57snxCrystal Structure of Benzamide Tetrahydro-4H-carbazol-4-one bound to Hsp903d0b290
582dd3-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as Inhibitors of the Hsp90 Molecular Chaperone2byi461
59592Complex of HSP90 ATPase domain with tropane derived inhibitors4awq479
604bcCrystal Structures of human HSP90alpha complexed with dihydroxyphenylpyrazoles1yc1680
612q8Identification of novel HSP90/isoform selective inhibitors using structure-based drug design. Demonstration of potential utility in treating CNS disorders such as Huntington's disease4o04690
622d9HUMAN HSP90 WITH 4-CHLORO-6-(4-(4-(4-METHANESULPHONYL-BENZYL)- PIERAZIN-1-YL)-1H-PYRAZOL-3-YL)-BENZENE-1,3-DIOL2ccu740
63zz5Orally Active 2-Amino Thienopyrimidine Inhibitors of the Hsp90 Chaperone2wi5900
643jcCrystal Structure of Hsp90-alpha N-domain Bound to the Inhibitor NVP-HSP9904w7t900
65vj6Synthesis of Benzoquinone-Ansamycin-Inspired Macrocyclic Lactams from Shikimic Acid4jql1000
66c0yStructure of HSP90 with small molecule inhibitor bound2xht1100
67ykbTricyclic series of Hsp90 inhibitors2ykb1100
68ykeTricyclic series of Hsp90 inhibitors2yke1100
69gdmGELDANAMYCIN BOUND TO THE HSP90 GELDANAMYCIN-BINDING DOMAIN1yet1200
70zz4Orally Active 2-Amino Thienopyrimidine Inhibitors of the Hsp90 Chaperone2wi41560
71a94HSP90 complexed with A9430372qg01900
724bhHUMAN HSP90 WITH 4-CHLORO-6-(4-PIPERAZIN-1-YL-1H-PYRAZOL-3-YL)- BENZENE-1,2-DIOL2ccs2000
736lvHuman HSP90 alpha N-terminal domain in complex with an Aminotriazoloquinazoline inhibitor4cwn2600
74a91HSP90 complexed with A9179852qg24000
75puzHuman Hsp90-alpha with 8-(2,5-dimethoxy-benzyl)-2-fluoro-9-pent-9H-purin-6-ylamine1uyi4100
76t62Human HSP90 alpha N-terminal domain in complex with an Aminotriazoloquinazoline inhibitor4cwo6100
77yjwTricyclic series of Hsp90 inhibitors2yjw7600
782e1HUMAN HSP90 WITH 5-(5-CHLORO-2,4-DIHYDROXY-PHENYL)-4-PIPERAZIN-1-YL- 2H-PYRAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE2cct9500
79pu0Human Hsp90-alpha with 9-Butyl-8-(2,5-dimethoxy-benzyl)-2-fluoro-9H-purin-6-ylamine1uyh1.43e+004
80pu6Human Hsp90-alpha with 8-Benzo[1,3]dioxol-,5-ylmethyl-9-butyl-9H-purin-6-ylamine1uy91.53e+004
81puxHuman Hsp90-alpha with 8-Benzo[1,3]dioxol-,5-ylmethyl-9-butyl-2-fluoro-9H-purin-6-ylamine1uyk1.71e+004
82pu1Human Hsp90-alpha with 8-(2-chloro-3,4,5-trimethoxy-benzyl)-2-fluoro-9-pent-4-ylnyl-9H-purin-6-ylamine1uyf3e+004
83h05Human HSP90 alpha N-terminal domain in complex with an Aminotriazoloquinazoline inhibitor4cwf3.24e+004
84pu7Human Hsp90-alpha with 9-Butyl-8-(2,5-dimethoxy-benzyl)-9H-purin-6-ylamine1uyc4.1e+004
85pu2Human Hsp90-alpha with 8-(2,5-dimethoxy-benzyl)-2-fluoro-9H-purin-6-ylamine1uyg5.35e+004
86pu5Human Hsp90-alpha with 9-Butyl-8-(3-trimethoxy-benzyl)-9H-purin-6ylamine1uy87.5e+004
87pu4Human Hsp90-alpha with 9-Butyl-8-(4-methoxy-benzyl)-9H-purin-6-ylamine1uy72e+005
88pu8Human Hsp90-alpha with 9-Butyl-8-(2-chloro-3,4,5-trimethoxy-benzyl)-9H-purin-6-ylamine1uyd2e+005
89pu9Human Hsp90-alpha with 8-(2-chloro-3,4,5-trimethoxy-benzyl)-9-pent-4-ylnyl-9H-purin-6-ylamine1uye2e+005
90pu3Human Hsp90-alpha with 9-Butyl-8-(3,4,5-trimethoxy-benzyl)-9H-purin-6-ylamine1uy62e+005
91tqlDynamic Undocking and the Quasi-Bound State as tools for Drug Design5fnf7e+005
922dlStructure of HSP90 with small molecule inhibitor bound2xdl7.9e+005