BP 897 [Ligand Id: 7625] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL25236 (BP-897) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Displacement of [3H]-prazosin from human ADRA1A receptor | B | 8.04 | pKi | 9.15 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 885-888 [PMID:26723530] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Displacement of [3H]MK912 from human alpha2A receptor after 60 mins | B | 8.56 | pKi | 2.75 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5199-5202 [PMID:20656482] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
| ChEMBL | Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding | B | 7.08 | pKi | 83 | nM | Ki | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement. | B | 6.12 | pKi | 760 | nM | Ki | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane | B | 6.12 | pKi | 760 | nM | Ki | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement. | B | 5.52 | pKi | 3000 | nM | Ki | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D2 long receptor expressed in CHO cells | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| ChEMBL | Binding affinity for human Dopamine receptor D2 (short) by [3H]- spiperone displacement. | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Binding affinity for human Dopamine receptor D2 (long) by [3H]- spiperone displacement. | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Binding affinity to dopamine D2 | B | 6.68 | pKi | 208.93 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
| ChEMBL | Displacement of [3H]spiperone from human D2 short receptor expressed in CHO cells | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| ChEMBL | Displacement of [3H]-spiperone from human dopamine D2S receptor expressed in HEK293 cell membranes | B | 6.73 | pKi | 186 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 885-888 [PMID:26723530] |
| ChEMBL | Displacement of [3H]spiperone from human D2 receptor transfected in HEK293 cell membrane measured after 50 mins by competitive radioligand binding analysis | B | 7.16 | pKi | 69 | nM | Ki | Bioorg Med Chem Lett (2021) 48: 128269-128269 [PMID:34284107] |
| ChEMBL | Inhibition of [3H]YM-09151-2 binding to human Dopamine D2 receptor expressed in CHO cells | B | 7.21 | pKi | 61 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
| ChEMBL | Binding affinity for human dopamine receptor D2 by displacing [125I]iodosulpiride expressed in CHO cells | B | 7.21 | pKi | 61 | nM | Ki | J Med Chem (2003) 46: 3883-3899 [PMID:12930150] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2S receptor expressed in HEK cells | B | 7.28 | pKi | 52 | nM | Ki | Bioorg Med Chem (2007) 15: 7258-7273 [PMID:17826096] |
| ChEMBL | Displacement of [125I]-IABN from human dopamine D2L receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 7.47 | pKi | 33.6 | nM | Ki | J Med Chem (2011) 54: 3581-3594 [PMID:21495689] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Binding affinity for rat striatum Dopamine receptor D2 by [3H]spiperone displacement. | B | 7.21 | pKi | 61 | nM | Ki | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| Dopamine D3 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304406] [UniProtKB: P52703] | ||||||||
| ChEMBL | Effective concentration for Dopamine receptor D3 was determined in monkeys | F | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2003) 46: 3883-3899 [PMID:12930150] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay | F | 7.8 | pKd | 15.85 | nM | Kd | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) | F | 8 | pKi | <10 | nM | Ki | Bioorg Med Chem Lett (2021) 48: 128269-128269 [PMID:34284107] |
| ChEMBL | Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
| ChEMBL | Binding affinity for human Dopamine receptor D3 by [3H]- spiperone displacement. | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor by liquid scintillation counting | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2009) 17: 758-766 [PMID:19081257] |
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor transfected in HEK293 cell membrane measured after 50 mins by competitive radioligand binding analysis | B | 8.9 | pKi | 1.27 | nM | Ki | Bioorg Med Chem Lett (2021) 48: 128269-128269 [PMID:34284107] |
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | Nature (1999) 400: 371-5 [PMID:10432116] |
| ChEMBL | Binding affinity for human dopamine receptor D3 by displacing [125I]iodosulpiride expressed in CHO cells | B | 9.04 | pKi | 0.92 | nM | Ki | J Med Chem (2003) 46: 3883-3899 [PMID:12930150] |
| ChEMBL | Inhibition of [3H]YM-09151-2 binding to human Dopamine D3 receptor expressed in CHO cells | B | 9.04 | pKi | 0.92 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | B | 9.04 | pKi | 0.91 | nM | Ki | Bioorg Med Chem (2007) 15: 7258-7273 [PMID:17826096] |
| ChEMBL | Displacement of [3H]-spiperone from human dopamine D3 receptor expressed in CHO cell membranes | B | 9.17 | pKi | 0.67 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 885-888 [PMID:26723530] |
| ChEMBL | Displacement of [125I]-IABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2011) 54: 3581-3594 [PMID:21495689] |
| ChEMBL | Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3 | F | 7.25 | pIC50 | 56 | nM | IC50 | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
| ChEMBL | Partial agonist intrinsic activity at dopamine D3 receptor | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
| ChEMBL | Mitogenic stimulation in CHO cells expressing human Dopamine receptor D3 | F | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
| ChEMBL | Mitogenic stimulation in NG 108-15 cells expressing human D3 receptor | F | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
| ChEMBL | Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from rat dopamine D3 receptor after 60 mins | B | 7.69 | pKi | 20.2 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5199-5202 [PMID:20656482] |
| ChEMBL | Binding affinity D3 [3H]-PD 128907 receptor was determined using caudate-putamen of adult male Spragueo?=Dawley rats | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1701-1705 [PMID:15745825] |
| ChEMBL | Binding affinity towards dopamine D3 receptor in ventral striatal membranes of sprague-dawley rat brain by using [3H]-PD 128907 as radioligand | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5813-5816 [PMID:15501046] |
| ChEMBL | Inhibition of [3H]-PD 128907 binding to Dopamine receptor D3 in rat ventral striatum | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2005) 48: 3171-3181 [PMID:15857123] |
| ChEMBL | Binding affinity for rat striatum Dopamine receptor D3 (sf9 cells) by [3H]7-OH-DPAT displacement. | B | 9.04 | pKi | 0.92 | nM | Ki | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
| ChEMBL | Displacement of [3H]spiperone from human D4 receptor expressed in CHO cells | B | 7.36 | pKi | 44 | nM | Ki | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| ChEMBL | Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement. | B | 7.41 | pKi | 39 | nM | Ki | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane | B | 7.41 | pKi | 38.9 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
| D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| ChEMBL | Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane | B | 6.79 | pKi | 162 | nM | Ki | J Med Chem (2005) 48: 3171-3181 [PMID:15857123] |
| D5 receptor/Dopamine D5 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2281] [GtoPdb: 218] [UniProtKB: P25115] | ||||||||
| ChEMBL | Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain | B | 6.2 | pKi | 636 | nM | Ki | J Med Chem (2005) 48: 3171-3181 [PMID:15857123] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.7 | pIC50 | 1995.26 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]8OH-DPAT from human 5HT1A receptor after 60 mins | B | 6.76 | pKi | 174 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5199-5202 [PMID:20656482] |
| ChEMBL | Displacement of [3H]- 8-OH-DPAT from porcine 5-hydroxytryptamine 1A receptor | B | 7.09 | pKi | 81 | nM | Ki | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor of porcine cortical membrane | B | 7.09 | pKi | 81 | nM | Ki | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity for rat hippocampus 5-hydroxytryptamine 1A receptor by inhibition of [3H]8-OH-DPAT binding | B | 7.08 | pKi | 84 | nM | Ki | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting | B | 7.48 | pKi | 33.1 | nM | Ki | J Med Chem (2010) 53: 7573-7586 [PMID:20958049] |
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]
