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 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]