compound 21 [PMID: 22802221] [Ligand Id: 6918] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL189568 (Buloxibutid, Compound 21, T2 agonist compound 21) |
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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 [125-I]-[Sar1Ile8]-angiotensin II from human AT2R expressed in HEK293 cell membrane assessed as inhibition constant by radioligand binding assay | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem (2022) 66: 116804-116804 [PMID:35576659] |
| ChEMBL | Agonist activity at AT2 receptor in HEK293 cells | F | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem (2022) 65: 116790-116790 [PMID:35550979] |
| 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 (unknown origin) | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2018) 61: 9811-9840 [PMID:29969256] |
| 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 | 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] |
| 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] |
| ChEMBL | Displacement of [I125I]AngII form pig AT2 receptor myometrial membrane incubated for 1.5 hrs by gamma counting method | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem (2022) 65: 116790-116790 [PMID:35550979] |
| 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] |
| ChEMBL | Displacement of 125I-[Sar1,Ile8]ANGII form recombinant human full length AT1 receptor expressed in HEK293 cells incubated for 120 mins by scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2022) 65: 116790-116790 [PMID:35550979] |
| 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 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]
