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 receptor A1 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 receptor A1 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 receptor A2a 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 receptor A2a 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 receptor A2b 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 receptor A3 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 | Agonist activity at human GPR18 expressed in CHO cells assessed as activation by measuring beta-arrestin2 recruitment incubated for 90 mins by luminescence based assay | F | 6.25 | pEC50 | 562 | nM | EC50 | J Med Chem (2024) 67: 9896-9926 [PMID:38885438] |
| GPR18/N-arachidonyl glycine receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6066225] [GtoPdb: 89] [UniProtKB: Q8K1Z6] | ||||||||
| ChEMBL | Agonist activity at mouse GPR18 expressed in CHO cells assessed as activation by measuring beta-arrestin2 recruitment incubated for 90 mins by luminescence based assay | B | 5.75 | pEC50 | 1780 | nM | EC50 | J Med Chem (2024) 67: 9896-9926 [PMID:38885438] |
ChEMBL data shown on this page come from version 36:
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]
