compound 21 [PMID: 22802221] [Ligand Id: 6918] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL189568
  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
  • AT2 receptor in Rat [GtoPdb: 35] [UniProtKB: P35351]
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  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
  • Type-1 angiotensin II receptor in Pig [ChEMBL: CHEMBL5743] [UniProtKB: P30555]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
ChEMBL Displacement of [125I]CGP-42112A from human AT2 receptor expressed in HEK293 cells B 8.01 pKi 9.8 nM Ki Bioorg Med Chem Lett (2014) 24: 476-479 [PMID:24388688]
ChEMBL Displacement of [125I]-Ang II from pig uterus membrane angiotensin II type 2 (AT2) receptor B 9.4 pKi 0.4 nM Ki J Med Chem (2004) 47: 5995-6008 [PMID:15537354]
ChEMBL Binding affinity to AT2 receptor B 9.4 pKi 0.4 nM Ki Bioorg Med Chem (2010) 18: 4570-4590 [PMID:20493713]
ChEMBL Binding affinity to AT2 receptor (unknown origin) B 9.4 pKi 0.4 nM Ki ACS Med Chem Lett (2014) 5: 1129-1132 [PMID:25313325]
ChEMBL Binding affinity to type-2 angiotensin-2 receptor (unknown origin) B 9.4 pKi 0.4 nM Ki Bioorg Med Chem Lett (2016) 26: 1355-1359 [PMID:26810314]
ChEMBL Binding affinity to AT2 receptor (unknown origin) B 9.4 pKi 0.4 nM Ki J Med Chem (2018) 61: 9811-9840 [PMID:29969256]
GtoPdb - - 9.4 pKi 0.4 nM Ki J Med Chem (2004) 47: 5995-6008 [PMID:15537354]
GtoPdb - - 4.8 pEC50 - - - Hypertension (2012) 60: 722-9 [PMID:22802221]
AT2 receptor in Rat [GtoPdb: 35] [UniProtKB: P35351]
GtoPdb - - 5.8 pEC50 - - - Hypertension (2012) 60: 722-9 [PMID:22802221]
Angiotensin type II receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163122] [UniProtKB: Q2XUH7]
ChEMBL Displacement of [125I]angiotensin 2 from AT2 receptor in pig uterus membrane after 1.5 hrs by gamma counting B 9.4 pKi 0.4 nM Ki Bioorg Med Chem (2010) 18: 4570-4590 [PMID:20493713]
ChEMBL Binding affinity to pig AT2 receptor B 9.4 pKi 0.4 nM Ki Bioorg Med Chem Lett (2014) 24: 476-479 [PMID:24388688]
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
ChEMBL Displacement of [125]Ang2 from AT1 receptor in rat liver membrane B 5 pKi >10000 nM Ki Bioorg Med Chem (2008) 16: 6841-6849 [PMID:18599297]
ChEMBL Displacement of [125I]-Ang II from AT1 receptor in rat liver membranes after 2 hrs by gamma-counting method B 5 pKi >10000 nM Ki ACS Med Chem Lett (2015) 6: 178-182 [PMID:25699147]
ChEMBL Displacement of [125I]Ang II from AT1 receptor in rat liver membranes B 5 pKi >10000 nM Ki J Med Chem (2020) 63: 1978-1995 [PMID:32030982]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Binding affinity to AT1 receptor B 5 pKi >10000 nM Ki Bioorg Med Chem (2010) 18: 4570-4590 [PMID:20493713]
ChEMBL Binding affinity to AT1 receptor (unknown origin) B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2014) 24: 476-479 [PMID:24388688]
ChEMBL Binding affinity to AT1 receptor (unknown origin) B 5 pKi >10000 nM Ki ACS Med Chem Lett (2014) 5: 1129-1132 [PMID:25313325]
ChEMBL Binding affinity to AT1 receptor (unknown origin) B 5 pKi 10000 nM Ki J Med Chem (2018) 61: 9811-9840 [PMID:29969256]
Type-1 angiotensin II receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5743] [UniProtKB: P30555]
ChEMBL Displacement of [125]Ang2 from AT2 receptor in pig uterus membrane B 9.4 pKi 0.4 nM Ki Bioorg Med Chem (2008) 16: 6841-6849 [PMID:18599297]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]