ChEMBL ligand: CHEMBL467399 (Biib021, BIIB 021, BIIB-021, Cnf-2024, Cnf2024, CNF2024)
heat shock protein 90 beta family member 1/Endoplasmin in Human [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625] There should be some charts here, you may need to enable JavaScript!
TNF receptor associated protein 1/Heat shock protein 75 kDa, mitochondrial in Human [ChEMBL: CHEMBL1075132] [GtoPdb: 2909] [UniProtKB: Q12931] There should be some charts here, you may need to enable JavaScript!
Heat shock protein 90 beta in Dog [ChEMBL: CHEMBL4748] [UniProtKB: P41148] There should be some charts here, you may need to enable JavaScript!
heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900] There should be some charts here, you may need to enable JavaScript!
heat shock protein 90 alpha family class B member 1/Heat shock protein HSP 90-beta in Human [ChEMBL: CHEMBL4303] [GtoPdb: 2907] [UniProtKB: P08238] There should be some charts here, you may need to enable JavaScript!
coactivator associated arginine methyltransferase 1 in Human [GtoPdb: 1255] [UniProtKB: Q86X55] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
heat shock protein 90 beta family member 1/Endoplasmin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625]
ChEMBL	Binding affinity to human N-terminal polyHis-tagged GRP94 (L69 to N337) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay	B	6.75	pKi	176	nM	Ki	Bioorg Med Chem Lett (2014) 24: 204-208 [PMID:24332488]
TNF receptor associated protein 1/Heat shock protein 75 kDa, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075132] [GtoPdb: 2909] [UniProtKB: Q12931]
ChEMBL	Binding affinity to human recombinant TRAP1 after 3 hrs by fluorescence polarization assay	B	7.21	pKi	62	nM	Ki	Bioorg Med Chem Lett (2014) 24: 204-208 [PMID:24332488]
ChEMBL	Inhibition of FITC3-labeled PU-H71 binding to recombinant human N-terminal His6-tagged TRAP1 (60 to 561 residues) expressed in Escherichia coli BL21(DE3) after 24 hrs by fluorescence polarization assay	B	6.27	pIC50	535	nM	IC50	J Med Chem (2017) 60: 7569-7578 [PMID:28816449]
ChEMBL	Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant human Trap-1 after 24 hrs by fluorescence polarization assay	B	7.05	pIC50	90	nM	IC50	J Med Chem (2013) 56: 6803-6818 [PMID:23965125]
Heat shock protein 90 beta in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4748] [UniProtKB: P41148]
ChEMBL	Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from dog Grp94 after 24 hrs by fluorescence polarization assay	B	6.91	pIC50	124	nM	IC50	J Med Chem (2013) 56: 6803-6818 [PMID:23965125]
heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900]
ChEMBL	Binding affinity to CM5 sensor chip immobilized human HSP90alpha assessed as dissociation constant by SPR analysis	B	6.74	pKd	180	nM	Kd	J Med Chem (2023) 66: 733-751 [PMID:36574496]
ChEMBL	Binding affinity to human N-terminal polyHis-tagged HSP90alpha (D9 to E236) alpha-helix conformation expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay	B	8.7	pKi	2	nM	Ki	Bioorg Med Chem Lett (2014) 24: 204-208 [PMID:24332488]
ChEMBL	Inhibition of HSP90alpha	B	8.77	pKi	1.7	nM	Ki	J Med Chem (2010) 53: 3-17 [PMID:20055425]
ChEMBL	Binding affinity at recombinant Hsp90alpha incubated for 16 hrs by fluorescence polarization competition assay	B	8.77	pKi	1.7	nM	Ki	J Med Chem (2012) 55: 7786-7795 [PMID:22938030]
ChEMBL	Inhibition of recombinant human full-length C-terminal Hsi-tagged HSP90alpha (1 to 732 residues) expressed in Escherichia coli measured after 2 to 3 hrs by FITC-labeled geldanamycin probe based fluorescence polarization assay	B	4.25	pIC50	56800	nM	IC50	Eur J Med Chem (2020) 203: 112540-112540 [PMID:32683166]
ChEMBL	Inhibition of FITC-geldanamycin binding to HSP90alpha (unknown origin) after 3 hrs by fluorescence polarization assay	B	7.18	pIC50	65.7	nM	IC50	Eur J Med Chem (2018) 150: 667-677 [PMID:29567459]
ChEMBL	Inhibition of HSP90a (unknown origin)	B	7.18	pIC50	65.7	nM	IC50	Eur J Med Chem (2020) 190: 112086-112086 [PMID:32058238]
ChEMBL	Inhibition of FITC3-labeled PU-H71 binding to recombinant HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay	B	7.28	pIC50	52	nM	IC50	J Med Chem (2017) 60: 7569-7578 [PMID:28816449]
ChEMBL	Inhibition of FITC-labeled geldanamycin binding to human Hsp90alpha by fluorescence polarization assay	B	7.54	pIC50	29	nM	IC50	Bioorg Med Chem Lett (2017) 27: 237-241 [PMID:27914802]
ChEMBL	Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay	B	7.72	pIC50	19	nM	IC50	J Med Chem (2013) 56: 6803-6818 [PMID:23965125]
ChEMBL	Inhibition of Hsp90alpha	B	8.29	pIC50	5.1	nM	IC50	J Med Chem (2012) 55: 7786-7795 [PMID:22938030]
GtoPdb	-	-	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2014) 24: 204-8 [PMID:24332488]
ChEMBL	Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2	B	7.42	pEC50	38	nM	EC50	J Med Chem (2012) 55: 7786-7795 [PMID:22938030]
heat shock protein 90 alpha family class B member 1/Heat shock protein HSP 90-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4303] [GtoPdb: 2907] [UniProtKB: P08238]
ChEMBL	Binding affinity to Hsp90 nucleotide binding domain	B	8.77	pKd	1.7	nM	Kd	J Med Chem (2010) 53: 7280-7286 [PMID:20608738]
ChEMBL	Binding affinity to HSP90 under non-reducing conditions in absence of TECP	B	7.59	pKi	26	nM	Ki	J Med Chem (2010) 53: 3-17 [PMID:20055425]
ChEMBL	Binding affinity to HSP90 under reducing conditions in presence of TECP	B	7.89	pKi	13	nM	Ki	J Med Chem (2010) 53: 3-17 [PMID:20055425]
ChEMBL	Binding affinity to human N-terminal polyHis-tagged HSP90beta (D9 to E236) expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2014) 24: 204-208 [PMID:24332488]
ChEMBL	Binding affinity to HSP90 by fluorescence polarization assay	B	8.77	pKi	1.7	nM	Ki	J Med Chem (2010) 53: 3-17 [PMID:20055425]
ChEMBL	Binding affinity to Hsp90 nucleotide binding domain in human BT474 cells	B	6.85	pIC50	140	nM	IC50	J Med Chem (2010) 53: 7280-7286 [PMID:20608738]
ChEMBL	Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells	B	7.42	pIC50	38	nM	IC50	J Med Chem (2010) 53: 3-17 [PMID:20055425]
ChEMBL	Inhibition of Hsp90 assessed as Her2 degradation by cell based assay	B	7.52	pIC50	30	nM	IC50	Bioorg Med Chem (2009) 17: 2225-2235 [PMID:19017562]
ChEMBL	Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant HSP90beta (unknown origin) after 24 hrs by fluorescence polarization assay	B	7.77	pIC50	17	nM	IC50	J Med Chem (2013) 56: 6803-6818 [PMID:23965125]
ChEMBL	Inhibition of HSP90-mediated client protein HER2 degradation	B	8.15	pIC50	7	nM	IC50	J Med Chem (2010) 53: 3-17 [PMID:20055425]
coactivator associated arginine methyltransferase 1 in Human [GtoPdb: 1255] [UniProtKB: Q86X55]
GtoPdb	In vitro methylation of H3 (1-25).	-	8	pIC50	<10	nM	IC50	TP-064 A Chemical Probe For PRMT4. thesgc.org

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]