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ChEMBL ligand: CHEMBL445102 (L-741626) |
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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 | Displacement of [3H]SCH23390 from dopamine D1 receptor | B | 6.14 | pKi | 722 | nM | Ki | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [125I]IABN from human dopamine D2L receptor expressed in HEK293 cells | B | 7.95 | pKi | 11.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 745-749 [PMID:17095222] |
ChEMBL | Displacement of [125I]IABN from human dopamine D2L receptor expressed in HEK293 cells | B | 7.95 | pKi | 11.2 | nM | Ki | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting | B | 7.95 | pKi | 11.2 | nM | Ki | Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177] |
ChEMBL | Displacement of [125I]ABN from human dopamine D2 long receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439] |
ChEMBL | Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK cell membrane after 90 mins by scintillation counting analysis | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2014) 57: 3450-3463 [PMID:24666157] |
GtoPdb | - | - | 8.5 | pKi | - | - | - |
J Med Chem (1996) 39: 1941-2 [PMID:8642550]; Bioorg Med Chem Lett (2007) 17: 745-9 [PMID:17095222] |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | Antagonist activity at dopamine D2 receptor | F | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
ChEMBL | Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis | F | 8.35 | pEC50 | 4.46 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 745-749 [PMID:17095222] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Displacement of [125I]IABN from human dopamine D3 receptor expressed in HEK293 cells | B | 6.79 | pKi | 163 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 745-749 [PMID:17095222] |
ChEMBL | Displacement of [125I]IABN from human dopamine D3 receptor expressed in HEK293 cells | B | 6.79 | pKi | 163 | nM | Ki | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
ChEMBL | Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 6.98 | pKi | 104 | nM | Ki | Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439] |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 7 | pKi | 100 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | Compound was measured for its ability to compete with [3H]spiperone binding to the human Dopamine receptor D3 transfected in CHO cells | B | 7.06 | pKi | 87 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
ChEMBL | Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
ChEMBL | Displacement of [3H]methylspiperone from human D3 receptor expressed in HEK293 cell membrane after 90 mins by scintillation counting analysis | B | 7.31 | pKi | 48.6 | nM | Ki | J Med Chem (2014) 57: 3450-3463 [PMID:24666157] |
ChEMBL | Antagonist activity at dopamine D3 receptor | F | 7.04 | pIC50 | 90.4 | nM | IC50 | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
ChEMBL | Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis | F | 7.04 | pEC50 | 90.4 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 745-749 [PMID:17095222] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting | B | 5.82 | pKi | 1520.7 | nM | Ki | Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177] |
ChEMBL | Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells | B | 5.82 | pKi | 1520 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 745-749 [PMID:17095222] |
ChEMBL | Displacement of [125I]IABN from human dopamine D4 receptor | B | 5.96 | pKi | 1100 | nM | Ki | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
ChEMBL | Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 6.35 | pKi | 449 | nM | Ki | Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439] |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 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 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 7G8 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | 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 | 5.1 | pIC50 | 7943.28 | 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 | 5.3 | pIC50 | 5011.87 | 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 | 5.4 | pIC50 | 3981.07 | 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 5HT1A receptor | B | 5.2 | pKi | 6300 | nM | Ki | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor | B | 6.16 | pKi | 695 | nM | Ki | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
GtoPdb | - | - | 6.5 | pKi | - | - | - | J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Displacement of [3H]mesulergine from 5HT2C receptor | B | 5.18 | pKi | 6570 | nM | Ki | J Med Chem (2008) 51: 6095-6109 [PMID:18774793] |
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 1 hr by liquid scintillation counting | B | 7.71 | pKi | 19.3 | nM | Ki | Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439] |
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
GtoPdb | - | - | 6.2 | pKi | - | - | - | J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410] |
ChEMBL data shown on this page come from version 32:
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]