L741742 [Ligand Id: 3302] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL444309 (L-741742)
  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines B 5.77 pKi >1700 nM Ki J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells B 5.77 pKi >1700 nM Ki J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells. B 5.77 pKi >1700 nM Ki J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL Inhibition of human dopamine D2 receptor B 5.77 pKi >1700 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Affinity to displace [3H]spiperone from cloned human Dopamine receptor D3 (hD3) stably expressed in HEK393 cell lines B 6.11 pKi 770 nM Ki J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells B 6.11 pKi 770 nM Ki J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells. B 6.11 pKi 770 nM Ki J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL Inhibition of human dopamine D3 receptor B 6.32 pKi 480 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines B 8.46 pKi 3.5 nM Ki J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL Binding affinity towards human dopamine receptor D4 B 8.46 pKi 3.5 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells B 8.46 pKi 3.5 nM Ki J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells. B 8.46 pKi 3.5 nM Ki J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
GtoPdb - - 8.5 pKi 3.16 nM Ki J Med Chem (1996) 39: 1943-5 [PMID:8642551]
ChEMBL Inhibition of human dopamine D4 receptor B 8.6 pKi 2.5 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]

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]