L745870 [Ligand Id: 3303] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267014
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/5-hydroxytryptamine receptor 1E in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D1 receptor/D(1A) dopamine receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D(1A) dopamine receptor in Bovine [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
  • D1 receptor/D(1A) dopamine receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D5 receptor/D(1B) dopamine receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
  • D5 receptor/D(1B) dopamine receptor in Rat [ChEMBL: CHEMBL2281] [GtoPdb: 218] [UniProtKB: P25115]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D(2) dopamine receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/D(3) dopamine receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor/D(4) dopamine receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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  • δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Inhibition of serotonin 5-HT1A receptor (unknown origin) B 5.11 pKi 7800 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL In vitro binding affinity to human 5-hydroxytryptamine 1A receptor B 5.18 pKi 6620.9 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity to cloned human 5-hydroxytryptamine 1B receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL In vitro binding affinity to human 5-hydroxytryptamine 1D receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
5-ht1e receptor/5-hydroxytryptamine receptor 1E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Binding affinity to cloned human 5-hydroxytryptamine 1E receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity to cloned human 5-hydroxytryptamine 2A receptor B 6.34 pKi 453 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
ChEMBL Inhibition of serotonin 5-HT2 receptor (unknown origin) B 6.7 pKi 200 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity to cloned human 5-hydroxytryptamine 2C receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Binding affinity to cloned human 5-hydroxytryptamine 5A receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL In vitro binding affinity to human 5-hydroxytryptamine 6 receptor B 5.78 pKi 1656.2 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL In vitro binding affinity to human 5-hydroxytryptamine 7 receptor B 6.65 pKi 226.3 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Inhibition of alpha1C adrenergic receptor (unknown origin) B 5.66 pKi 2200 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Inhibition of alpha1B adrenergic receptor (unknown origin) B 5.54 pKi 2900 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibition of alpha2A adrenergic receptor (unknown origin) B 6.77 pKi 170 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Inhibition of alpha2B adrenergic receptor (unknown origin) B 6.8 pKi 160 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Inhibition of alpha2C adrenergic receptor (unknown origin) B 6.64 pKi 230 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Inhibition of human dopamine D1 receptor B 5 pKi >10000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D(1A) dopamine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1 B 5 pKi 9900 nM Ki Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement. B 5 pKi 9900 nM Ki Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL Displacement of [3H]SCH23390 from bovine dopamine D1 receptor B 5 pKi 9900 nM Ki Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
D1 receptor/D(1A) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL In vitro binding affinity to cloned rat Dopamine receptor D1 measured by displacement of radioligand [3H]SCH-23,982 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
D5 receptor/D(1B) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL Inhibition of human dopamine D5 receptor B 5 pKi >10000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D5 receptor/D(1B) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2281] [GtoPdb: 218] [UniProtKB: P25115]
ChEMBL In vitro binding affinity to cloned rat D5 receptor measured by displacement of radioligand [3H]SCH-23,982 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]-Spiperone displacement. B 4.27 pKi 54000 nM Ki Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL Displacement of [3H]SCH23390 from human cloned dopamine D2 long receptor expressed in CHO cells B 4.27 pKi 54000 nM Ki Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL Binding affinity to dopamine D2 B 4.27 pKi 53703.18 nM Ki J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL Displacement of [3H] Spiperone from human D2L receptor expressed in CHO cells by competitive radioligand binding assay B 4.33 pKi 47000 nM Ki J Med Chem (2019) 62: 9658-9679 [PMID:31613617]
ChEMBL In vitro binding affinity at human cloned dopamine receptor D2 (short) stably expressed in CHO cells by [3H]spiperone displacement. B 4.42 pKi 38000 nM Ki Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D2 short receptor expressed in CHO cells B 4.42 pKi 38000 nM Ki Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL Displacement of [3H] Spiperone from human D2S receptor expressed in CHO cells by competitive radioligand binding assay B 4.48 pKi 33000 nM Ki J Med Chem (2019) 62: 9658-9679 [PMID:31613617]
ChEMBL Displacement of 3H-N-Methylspiperone from DRD2 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 5.04 pKi 9120.11 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Displacement of 3H-N-Methylspiperone from DRD2 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 5.04 pKi 9111 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method B 5.79 pKi 1621.81 nM Ki J Med Chem (2022) 65: 12124-12139 [PMID:36098685]
ChEMBL Ability to displace [3H]spiperone from cloned human dopamine D2 receptor stably expressed in CHO cells B 6.02 pKi 960 nM Ki Bioorg Med Chem Lett (1999) 9: 585-588 [PMID:10098669]
ChEMBL Binding affinity to D2R (unknown origin) assessed as inhibition constant B 6.02 pKi 960 nM Ki Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL Inhibition of human dopamine D2 receptor B 6.02 pKi 960 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand B 6.02 pKi 960 nM Ki J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by PDSP assay B 6.02 pKi 960 nM Ki Bioorg Med Chem (2014) 22: 3105-3114 [PMID:24800940]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting B 6.02 pKi 960 nM Ki Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL In vitro binding affinity was measured at the cloned human Dopamine receptor D2 using [3H]spiroperidol as radioligand. B 6.04 pKi 920 nM Ki J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells B 6.04 pKi 908 nM Ki Bioorg Med Chem Lett (1998) 8: 1499-1502 [PMID:9873377]
ChEMBL Binding affinity at Dopamine receptor D2 in CHO cells by radioligand displacement. B 6.04 pKi 908 nM Ki J Med Chem (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL Binding affinity against human Dopamine receptor D2 using [3H]spiperone as radioligand B 6.35 pKi 448 nM Ki J Med Chem (2004) 47: 2348-2355 [PMID:15084133]
D(2) dopamine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Binding affinity was evaluated for the displacement of [3H]spiperone against bovine Dopamine receptor D2 B 5.21 pKi 6100 nM Ki Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
D2 receptor/D(2) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro binding affinity to rat Dopamine receptor D2 measured by displacement of the radioligand [3H]spiperone B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H] Spiperone from human D3 receptor expressed in CHO cells by competitive radioligand binding assay B 4.19 pKi 65000 nM Ki J Med Chem (2019) 62: 9658-9679 [PMID:31613617]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane B 4.51 pKi 30902.95 nM Ki J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL Binding affinity evaluated for the displacement of [3H]-spiperone against human dopamine receptor D3 B 4.54 pKi 29000 nM Ki Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL In vitro binding affinity at human cloned dopamine receptor D3 stably expressed in CHO cells by [3H]spiperone displacement. B 4.66 pKi 22000 nM Ki Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor expressed in CHO cells B 4.66 pKi 22000 nM Ki Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells B 5.52 pKi >3030 nM Ki Bioorg Med Chem Lett (1998) 8: 1499-1502 [PMID:9873377]
ChEMBL Binding affinity at Dopamine receptor D3 in CHO cells by radioligand displacement. B 5.52 pKi >3030 nM Ki J Med Chem (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL Inhibition of human dopamine D3 receptor B 5.64 pKi 2310 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL Binding affinity to D3R (unknown origin) assessed as inhibition constant B 5.64 pKi 2310 nM Ki Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL Ability to displace [3H]-spiperone from cloned human dopamine D3 receptor stably expressed in CHO cells B 5.64 pKi 2300 nM Ki Bioorg Med Chem Lett (1999) 9: 585-588 [PMID:10098669]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by PDSP assay B 5.64 pKi 2300 nM Ki Bioorg Med Chem (2014) 22: 3105-3114 [PMID:24800940]
ChEMBL Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand B 5.64 pKi 2300 nM Ki J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL Displacement of [3H]N-methylspiperone from human D3R receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method B 6.42 pKi 380.19 nM Ki J Med Chem (2022) 65: 12124-12139 [PMID:36098685]
D3 receptor/D(3) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL In vitro binding affinity to cloned rat Dopamine receptor D3 measured by displacement of the radioligand [3H]sulpiride B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of 3H-N-Methylspiperone from DRD4 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 8.56 pKi 2.78 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Displacement of 3H-N-Methylspiperone from DRD4 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 8.56 pKi 2.75 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method B 8.65 pKi 2.24 nM Ki J Med Chem (2018) 61: 3712-3725 [PMID:29589445]
ChEMBL Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method B 8.65 pKi 2.24 nM Ki J Med Chem (2022) 65: 12124-12139 [PMID:36098685]
ChEMBL In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement. B 9.04 pKi 0.91 nM Ki Bioorg Med Chem Lett (1998) 8: 1499-1502 [PMID:9873377]
ChEMBL Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement. B 9.04 pKi 0.91 nM Ki J Med Chem (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay B 9.15 pKi 0.7 nM Ki J Med Chem (2019) 62: 9658-9679 [PMID:31613617]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells B 9.21 pKi 0.62 nM Ki Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement. B 9.21 pKi 0.62 nM Ki Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane B 9.21 pKi 0.62 nM Ki J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL Ability to displace [3H]spiperone from dopamine receptor D4.4 expressed in CHO-K1 cells B 9.21 pKi 9.21 D4 Log Ki J Med Chem (2001) 44: 1151-1157 [PMID:11312915]
ChEMBL Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane B 9.22 pKi 0.6 nM Ki Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180]
ChEMBL Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4 B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane B 9.26 pKi 0.55 nM Ki Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180]
ChEMBL Binding affinity towards human dopamine receptor D4 B 9.37 pKi 0.43 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL In vitro binding affinity to human Dopamine receptor D4 B 9.37 pKi 0.43 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
ChEMBL In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand. B 9.37 pKi 0.43 nM Ki J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells B 9.37 pKi 0.43 nM Ki Bioorg Med Chem Lett (1999) 9: 585-588 [PMID:10098669]
ChEMBL Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting B 9.37 pKi 0.43 nM Ki Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL Inhibition of human dopamine D4 receptor B 9.37 pKi 0.43 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand B 9.37 pKi 0.43 nM Ki J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant B 9.37 pKi 0.43 nM Ki Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983]
ChEMBL Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement. B 9.4 pKi 0.4 nM Ki J Med Chem (2004) 47: 2348-2355 [PMID:15084133]
GtoPdb - - 9.41 pKi 0.39 nM Ki J Med Chem (1996) 39: 1941-2 [PMID:8642550]
ChEMBL Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay F 5.71 pIC50 1949.84 nM IC50 J Med Chem (2022) 65: 12124-12139 [PMID:36098685]
ChEMBL Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay F 6.79 pIC50 162.18 nM IC50 J Med Chem (2022) 65: 12124-12139 [PMID:36098685]
ChEMBL Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay F 6.84 pIC50 144.54 nM IC50 J Med Chem (2022) 65: 12124-12139 [PMID:36098685]
ChEMBL Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay B 7.03 pIC50 93.33 nM IC50 J Med Chem (2018) 61: 3712-3725 [PMID:29589445]
ChEMBL Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay B 7.37 pIC50 42.66 nM IC50 J Med Chem (2018) 61: 3712-3725 [PMID:29589445]
ChEMBL Effective concentration against human Dopamine receptor D4 B 5.65 pEC50 2230 nM EC50 J Med Chem (2004) 47: 2348-2355 [PMID:15084133]
ChEMBL Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay F 7.57 pEC50 27 nM EC50 Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
D4 receptor/D(4) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone B 8.43 pKi 3.7 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
ChEMBL Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay B 9.37 pKi 0.43 nM Ki Bioorg Med Chem (2014) 22: 3105-3114 [PMID:24800940]
δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Binding affinity to cloned Opioid receptor delta 1 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5]
ChEMBL Binding affinity for N-methyl-D-aspartate glutamate receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
ChEMBL Binding affinity to PCP site of rat N-methyl-D-aspartate glutamate receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity to cloned Histamine H1 receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity to cloned Opioid receptor kappa 1 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity to cloned Muscarinic acetylcholine receptor M1 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
ChEMBL Binding affinity to cloned Muscarinic acetylcholine receptor M2 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Binding affinity to cloned Muscarinic acetylcholine receptor M3 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Binding affinity to cloned Muscarinic acetylcholine receptor M4 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Binding affinity to cloned Muscarinic acetylcholine receptor M5 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Binding affinity to cloned Opioid receptor mu 1 B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Binding affinity towards sigma receptor was determined B 6.89 pKi 130 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H] Pentazocine from sigma 1 receptor in HEK293 cell membrane B 7 pKi 101 nM Ki Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180]
ChEMBL Displacement of [3H] Pentazocine from sigma 1 receptor in HEK293 cell membrane B 7 pKi 100 nM Ki Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180]

ChEMBL data shown on this page come from version 35:

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]