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] |
| FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR65 | F | 5.29 | pIC50 | 5070.89 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
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]
