[3H]SB269970 [Ligand Id: 3247] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL282199 (SB-269970)
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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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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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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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-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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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-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
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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]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
  • Serotonin 7 (5-HT7) receptor in Guinea pig [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity towards Alpha-1B adrenergic receptor B 5 pKi <10000 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity towards Dopamine receptor D2 (human cloned receptor) in CHO cells using [125I]iodosulpiride radioligand. B 6.5 pKi 316.23 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
ChEMBL Displacement of [3H]raclopride from human dopamine receptor D2A expressed in mouse Ltk cells B 6.5 pKi 316 nM Ki J Med Chem (2001) 44: 1337-1340 [PMID:11311055]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity towards Dopamine receptor D3 (human cloned receptor) in CHO cells using [125I]iodosulpiride radioligand. B 5.6 pKi 2511.89 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor (human cloned receptor) in HEK293 cells using [3H]8-OH-DPAT as radioligand; B 5 pKi <10000 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in CHO cells B 5 pKi >10000 nM Ki J Med Chem (2001) 44: 1337-1340 [PMID:11311055]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry B 5 pKi >10000 nM Ki Eur J Med Chem (2014) 85: 716-726 [PMID:25128671]
ChEMBL Antagonist activity at 5-HT1A receptor (unknown origin) B 5 pKi >10000 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
ChEMBL Binding affinity to 5HT1A receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Displacement of [3H]-8-OH-DPAT from recombinant human 5-HT1A receptor expressed in CHOK1 cell membranes after 1 hr by liquid scintillation counting method B 5.04 pKi 9024 nM Ki Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry B 5.04 pKi 9024 nM Ki Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505]
ChEMBL Displacement of [3H]-5-HT from human 5-HT1A receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis B 5.04 pKi 9024 nM Ki Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr B 5.3 pKi >5000 nM Ki Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells B 8.3 pKi <5 nM Ki Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity to 5HT1A receptor in rat hippocampus B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2009) 19: 4827-4831 [PMID:19560916]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity to 5HT1B receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand B 6 pKi 1000 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Binding affinity to 5HT1D receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Binding affinity towards human cloned 5-hydroxytryptamine 1D receptor in CHO cells using [3H]5-HT as radioligand. B 5.8 pKi 1584.89 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Binding affinity to 5HT1E receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Binding affinity towards human cloned 5-hydroxytryptamine 1E receptor in CHO cells using [3H]5-HT as radioligand. B 5.2 pKi <6309.57 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1F receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand. B 5.5 pKi <3162.28 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity towards 5-hydroxytryptamine 2A receptor (human cloned receptor) in HEK 293 cells using [3H]ketanserin as radioligand. B 5 pKi <10000 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in HEK293 cells B 8.3 pKi <5 nM Ki Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity to 5HT2A receptor in rat cortex B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2009) 19: 4827-4831 [PMID:19560916]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand B 5 pKi 10000 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
ChEMBL Binding affinity to 5HT2B receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor in HEK293 cells, using [3H]mesulergine as radioligand B 5 pKi <10000 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
ChEMBL Binding affinity to 5HT2C receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity to 5HT3 receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Binding affinity to 5HT4 receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Binding affinity towards 5-hydroxytryptamine 4 receptor B 5.9 pKi 1258.93 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Binding affinity towards 5-hydroxytryptamine 5 receptor B 7.19 pKi 65 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand. B 7.2 pKi 63.1 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
ChEMBL Binding affinity to 5HT5A receptor (unknown origin) B 9.11 pKi 0.78 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity to 5HT6 receptor (unknown origin) B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand. B 5.2 pKi 6309.57 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity to 5HT7 receptor B 8.01 pKd 9.7 nM Kd Eur J Med Chem (2011) 46: 3455-3461 [PMID:21620533]
GtoPdb - - 8.92 pKd 1.2 nM Kd Br J Pharmacol (2000) 130: 409-17 [PMID:10807680]
ChEMBL Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter B 8.72 pKi 1.9 nM Ki Eur J Med Chem (2019) 183: 111690-111690 [PMID:31526973]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 7 receptor B 8.89 pKi 1.3 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells B 8.89 pKi 1.3 nM Ki Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652]
ChEMBL Binding affinity to 5HT7 receptor (unknown origin) B 8.9 pKi 1.26 nM Ki Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835]
ChEMBL Binding affinity to human 5-HT7 receptor by radioligand binding assay B 8.9 pKi 1.26 nM Ki J Med Chem (2018) 61: 8475-8503 [PMID:29767995]
ChEMBL Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry B 8.9 pKi 1.26 nM Ki Eur J Med Chem (2014) 85: 716-726 [PMID:25128671]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells B 8.9 pKi 1.26 nM Ki Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652]
ChEMBL Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand. B 8.9 pKi 1.26 nM Ki J Med Chem (2000) 43: 342-345 [PMID:10669560]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand B 8.9 pKi 1.26 nM Ki J Med Chem (2003) 46: 5638-5650 [PMID:14667218]
ChEMBL Antagonist activity at 5-HT7 receptor (unknown origin) B 8.9 pKi 1.25 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting B 8.92 pKi 1.2 nM Ki Bioorg Med Chem (2011) 19: 6750-6759 [PMID:22001327]
ChEMBL Binding affinity to human cloned 5HT7 receptor expressed in HEK293 cells B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2009) 19: 4827-4831 [PMID:19560916]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr B 8.92 pKi 1.2 nM Ki Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL Binding affinity to 5HT7 receptor B 9 pKi 1 nM Ki Bioorg Med Chem Lett (2011) 21: 42-44 [PMID:21159507]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD B 9 pKi 1 nM Ki Bioorg Med Chem Lett (2002) 12: 2451-2454 [PMID:12161155]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis B 9.15 pKi 0.71 nM Ki Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032]
ChEMBL Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry B 9.15 pKi 0.71 nM Ki Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505]
ChEMBL Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method B 9.15 pKi 0.71 nM Ki Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784]
ChEMBL Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting B 9.47 pKi 0.34 nM Ki Eur J Med Chem (2016) 123: 180-190 [PMID:27475109]
ChEMBL Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method B 9.47 pKi 0.34 nM Ki J Med Chem (2018) 61: 7218-7233 [PMID:30028132]
ChEMBL Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method B 9.47 pKi 0.34 nM Ki Eur J Med Chem (2016) 110: 302-310 [PMID:26852005]
ChEMBL Displacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method B 9.47 pKi 0.34 nM Ki Bioorg Med Chem (2014) 22: 4587-4596 [PMID:25127461]
ChEMBL Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting B 9.47 pKi 0.34 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting B 9.47 pKi 0.34 nM Ki J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method B 9.47 pKi 0.34 nM Ki Eur J Med Chem (2016) 110: 302-310 [PMID:26852005]
ChEMBL Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method B 9.47 pKi 0.34 nM Ki J Med Chem (2018) 61: 7218-7233 [PMID:30028132]
ChEMBL Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay F 8.43 pIC50 3.71 nM IC50 Eur J Med Chem (2016) 123: 180-190 [PMID:27475109]
ChEMBL Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay F 8.43 pIC50 3.71 nM IC50 Eur J Med Chem (2016) 123: 180-190 [PMID:27475109]
ChEMBL Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay B 8.58 pIC50 2.63 nM IC50 Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay B 8.59 pIC50 2.6 nM IC50 Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay F 9.03 pIC50 0.93 nM IC50 J Med Chem (2018) 61: 7218-7233 [PMID:30028132]
ChEMBL Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis F 9.03 pIC50 0.93 nM IC50 J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
ChEMBL Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay F 9.03 pIC50 0.93 nM IC50 Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay F 9.05 pIC50 0.9 nM IC50 J Med Chem (2018) 61: 7218-7233 [PMID:30028132]
ChEMBL Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis F 9.3 pIC50 0.5 nM IC50 J Med Chem (2021) 64: 13766-13779 [PMID:34519505]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand. B 7.5 pKi 31.62 nM Ki J Med Chem (2003) 46: 5638-5650 [PMID:14667218]
ChEMBL Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells B 8.9 pKi 1.26 nM Ki J Med Chem (2001) 44: 1337-1340 [PMID:11311055]
ChEMBL Binding affinity towards rat 5-HT7 receptor expressed in HEK cells B 9 pKi 1 nM Ki J Med Chem (2004) 47: 5451-5466 [PMID:15481983]
Serotonin 7 (5-HT7) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
ChEMBL Antagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction F 7.48 pKd 33.11 nM Kd J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contraction F 7.48 pKd 33.11 nM Kd J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL Antagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction F 7.69 pKd 20.42 nM Kd J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Antagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction F 7.8 pKd 15.85 nM Kd J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Antagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction F 7.84 pKd 14.45 nM Kd J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction F 7.84 pKd 14.45 nM Kd J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction F 7.9 pKd 12.59 nM Kd J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL Antagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction F 7.96 pKd 10.96 nM Kd J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction F 8.05 pKd 8.91 nM Kd J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction F 8.1 pKd 7.94 nM Kd J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction F 8.2 pKd 6.31 nM Kd J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction F 8.4 pKd 3.98 nM Kd J Med Chem (2007) 50: 4214-4221 [PMID:17649988]

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]