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 Binding affinity to D2R (unknown origin) assessed as inhibition constant B 4.77 pKi >17000 nM Ki Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
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 Binding affinity to D3R (unknown origin) assessed as inhibition constant B 6.11 pKi 770 nM Ki Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
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]
ChEMBL Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant B 8.46 pKi 3.5 nM Ki Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
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 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]