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

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ChEMBL ligand: CHEMBL267014 (L-745870)
  • 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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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
  • D5 receptor/Dopamine D5 receptor in Rat [ChEMBL: CHEMBL2281] [GtoPdb: 218] [UniProtKB: P25115]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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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-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor 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
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]
δ receptor/Delta 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]
D1 receptor/Dopamine D1 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]
Dopamine D1 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/Dopamine D1 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]
D2 receptor/Dopamine D2 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 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 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] 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 Inhibition of human dopamine D2 receptor B 6.02 pKi 960 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
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 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 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 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]
Dopamine D2 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/Dopamine D2 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/Dopamine D3 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 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 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 Inhibition of human dopamine D3 receptor B 5.64 pKi 2310 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
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]
D3 receptor/Dopamine D3 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/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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 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 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 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 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]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 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 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 [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 human dopamine receptor D4 B 9.37 pKi 0.43 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
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 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 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 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/Dopamine D4 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]
D5 receptor/Dopamine D5 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/Dopamine D5 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]
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 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]
μ receptor/Mu 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]
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]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor 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/Serotonin 1b (5-HT1b) receptor 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/Serotonin 1d (5-HT1d) receptor 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/Serotonin 1e (5-HT1e) receptor 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/Serotonin 2a (5-HT2a) receptor 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/Serotonin 2c (5-HT2c) receptor 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/Serotonin 5a (5-HT5a) receptor 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/Serotonin 6 (5-HT6) receptor 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/Serotonin 7 (5-HT7) receptor 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]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor 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 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]