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 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]
