L 755507 [Ligand Id: 3931] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL12998 (L-755507)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • This target only has 1 pki data point
1 CHEMBL12998_lig_chart_1 Beta-1 adrenergic receptor Human
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • This target only has 1 pki data point
2 CHEMBL12998_lig_chart_2 Beta-2 adrenergic receptor Human
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
  • This target only has 0 pki data point
3 CHEMBL12998_lig_chart_3 Beta-3 adrenergic receptor Human
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  • Cruzipain in Trypanosoma cruzi [ChEMBL: CHEMBL3563] [UniProtKB: P25779]
  • This target only has 0 pki data point
4 CHEMBL12998_lig_chart_4 Cruzipain Trypanosoma cruzi
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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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]