L 755507 [Ligand Id: 3931] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL12998 (L-755507) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptors | B | 6.24 | pKi | 570 | nM | Ki | J Med Chem (2001) 44: 1456-1466 [PMID:11311069] |
| ChEMBL | In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol. | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1107-1112 [PMID:9871717] |
| ChEMBL | In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor | B | 6.48 | pEC50 | 330 | nM | EC50 | J Med Chem (2001) 44: 1456-1466 [PMID:11311069] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2001) 44: 1456-1466 [PMID:11311069] |
| ChEMBL | Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3087-3092 [PMID:9873681] |
| ChEMBL | In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol. | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1107-1112 [PMID:9871717] |
| ChEMBL | Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors | F | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2001) 44: 1456-1466 [PMID:11311069] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| ChEMBL | In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor. | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2001) 44: 1456-1466 [PMID:11311069] |
| ChEMBL | Evaluated for its agonist activity against human Beta-3 adrenergic receptor | F | 9.37 | pEC50 | 0.43 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 2111-2116 [PMID:9873496] |
| ChEMBL | Agonism against Beta-3 adrenergic receptor | F | 9.37 | pEC50 | 0.43 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 3087-3092 [PMID:9873681] |
| ChEMBL | Agonist activity towards human Beta-3 adrenergic receptor | F | 9.37 | pEC50 | 0.43 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1107-1112 [PMID:9871717] |
| ChEMBL | Binding affinity towards human Beta-3 adrenergic receptor | B | 9.37 | pEC50 | 0.43 | nM | EC50 | J Med Chem (1999) 42: 181-201 [PMID:9925722] |
| GtoPdb | - | - | 10.1 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779] | ||||||||
| ChEMBL | Inhibition of Trypanosoma cruzi cruzain by quantitative high throughput screening | B | 4.22 | pIC50 | >60000 | nM | IC50 | J Med Chem (2010) 53: 37-51 [PMID:19908840] |
| ChEMBL | Inhibition of Trypanosoma cruzi cruzain by Flexstation microplate spectrofluorimetry | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2010) 53: 37-51 [PMID:19908840] |
ChEMBL data shown on this page come from version 33:
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]
