L-162,313 [Ligand Id: 3936] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL288174 (L-162313) |
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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 | Binding affinity at Angiotensin II receptor, type 2 in pig uterus myometrial membranes by [125I]-Ang II displacement. | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (2004) 47: 1536-1546 [PMID:14998339] |
| ChEMBL | Displacement of [125I]-Ang II from pig uterus membrane angiotensin II type 2 (AT2) receptor | B | 8.55 | pKi | 2.8 | nM | Ki | J Med Chem (2004) 47: 5995-6008 [PMID:15537354] |
| ChEMBL | Displacement of 125I-[Sar1,Ile8]ANGII form AT2 receptor (unknown origin) | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem (2022) 65: 116790-116790 [PMID:35550979] |
| ChEMBL | Inhibitory concentration against towards Angiotensin II receptor, type 2 was measured through displacement of [125I]-Ang II in pig uterus myometrial membranes | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2004) 47: 1536-1546 [PMID:14998339] |
| ChEMBL | Inhibition of Angiotensin II receptor, type 2 | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1996) 39: 625-656 [PMID:8576904] |
| ChEMBL | Displacement of [125I]-Ang II from pig uterus membrane angiotensin II type 2 (AT2) receptor | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2004) 47: 5995-6008 [PMID:15537354] |
| ChEMBL | Displacement of [125-I]-[Sar1, Ile8]-angiotensin II from AT2R (unknown origin) by radioligand binding assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem (2022) 66: 116804-116804 [PMID:35576659] |
| AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351] | ||||||||
| ChEMBL | Displacement of [125I]angiotensin 2 from rat AT2 receptor expressed in african green monkey COS7 cells after 24 hrs | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem (2010) 18: 4570-4590 [PMID:20493713] |
| Angiotensin type II receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163122] [UniProtKB: Q2XUH7] | ||||||||
| ChEMBL | Displacement of [I125I]AngII form pig AT2 receptor myometrial membrane incubated for 1.5 hrs by gamma counting method | B | 8.55 | pKi | 2.8 | nM | Ki | Bioorg Med Chem (2022) 65: 116790-116790 [PMID:35550979] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| GtoPdb | - | - | 7.92 | pIC50 | 11.9 | nM | IC50 | J Biol Chem (1995) 270: 1493-6 [PMID:7829475] |
| AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095] | ||||||||
| ChEMBL | Displacement of [125I]Ang II from AT1 receptor in rat liver membranes | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2020) 63: 1978-1995 [PMID:32030982] |
| ChEMBL | Displacement of [I125I]AngII form AT1 receptor in rat liver membrane incubated for 1.5 hrs by gamma counting method | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem (2022) 65: 116790-116790 [PMID:35550979] |
| ChEMBL | Displacement of [125]Ang2 from AT1 receptor in rat liver membrane | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem (2008) 16: 6841-6849 [PMID:18599297] |
| AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| ChEMBL | Displacement of 125I-[Sar1,Ile8]ANGII form AT1 receptor (unknown origin) | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem (2022) 65: 116790-116790 [PMID:35550979] |
| GtoPdb | - | - | 7.92 | pIC50 | 11.9 | nM | IC50 | J Biol Chem (1995) 270: 1493-6 [PMID:7829475] |
| ChEMBL | Inhibition of Angiotensin II receptor, type 1 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (1996) 39: 625-656 [PMID:8576904] |
| ChEMBL | Displacement of [125-I]-[Sar1, Ile8]-angiotensin II from AT1R (unknown origin) by radioligand binding assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem (2022) 66: 116804-116804 [PMID:35576659] |
| 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 | 8.7 | pKi | 2 | 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]
