PSB-KD107 [Ligand Id: 11081] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL239232 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells | B | 4.6 | pKi | >25000 | nM | Ki | Bioorg Med Chem (2007) 15: 6956-6974 [PMID:17827019] |
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane | B | 4.6 | pKi | 25000 | nM | Ki | Bioorg Med Chem (2007) 15: 6956-6974 [PMID:17827019] |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Displacement of [3H]MSX2 from human adenosine A2A receptor expressed in CHO cells | B | 5.34 | pKi | 4560 | nM | Ki | Bioorg Med Chem (2007) 15: 6956-6974 [PMID:17827019] |
| A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
| ChEMBL | Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatal membrane | B | 6.48 | pKi | 330 | nM | Ki | Bioorg Med Chem (2007) 15: 6956-6974 [PMID:17827019] |
| A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| ChEMBL | Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells | B | 5 | pKi | 10000 | nM | Ki | Bioorg Med Chem (2007) 15: 6956-6974 [PMID:17827019] |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Displacement of [3H]PSB11 from human adenosine A3 receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2007) 15: 6956-6974 [PMID:17827019] |
| GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6] | ||||||||
| ChEMBL | Antagonist activity at Prolink1-tagged human GPR55 receptor expressed in CHO cells assessed as inhibition of lysophosphatidylinositol-induced beta arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis | F | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2024-2031 [PMID:33062188] |
| ChEMBL | Agonist activity at Prolink1-tagged human GPR55 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis | B | 5 | pEC50 | >10000 | nM | EC50 | ACS Med Chem Lett (2020) 11: 2024-2031 [PMID:33062188] |
| GPR18/N-arachidonyl glycine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2384898] [GtoPdb: 89] [UniProtKB: Q14330] | ||||||||
| ChEMBL | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment by measuring 2-(3-(6-(4-chlorophenoxy)hexyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one IC50 at 1 uM after 90 mins by beta-galactosidase based topcount luminescence analysis | B | 6.03 | pIC50 | 944 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2024-2031 [PMID:33062188] |
| GtoPdb | - | - | 6.25 | pEC50 | 562 | nM | EC50 | ACS Medicinal Chemistry Letters (2020) : |
| ChEMBL | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis | B | 6.25 | pEC50 | 562 | nM | EC50 | ACS Med Chem Lett (2020) 11: 2024-2031 [PMID:33062188] |
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]
