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ChEMBL ligand: CHEMBL3421729 (Ly3154207, LY-3154207, LY3154207, Mevidalen) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
ChEMBL | Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 8.64 | pEC50 | 2.3 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
GtoPdb | Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC20 concentration of dopamine in HEK293 cells transiently expressing human D1 receptors. | - | 8.64 | pEC50 | 2.3 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
ChEMBL | Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay | F | 8.95 | pEC50 | 1.11 | nM | EC50 | J Med Chem (2019) 62: 128-140 [PMID:30525590] |
D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
ChEMBL | Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 7.21 | pEC50 | 62.1 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
GtoPdb | Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC20 concentration of dopamine in HEK293 cells transiently expressing mouse D1 receptors. | - | 7.21 | pEC50 | 62 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
ChEMBL | Positive allosteric modulator activity at human D5 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity to 5-HT1A receptor (unknown origin) by radioligand displacement assay | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
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]