L-741,626 [Ligand Id: 177] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL445102 (L-741626)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]