[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 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]