[3H]NGD941 [Ligand Id: 3297] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL103772 ([3H]NGD-941)
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT3A/5-hydroxytryptamine receptor 3A in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor B 6.74 pKi 181 nM Ki J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL Inhibition of serotonin 5-HT1A receptor (unknown origin) B 6.74 pKi 180 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Inhibition of serotonin 5-HT3 receptor (unknown origin) B 6.12 pKi 750 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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 5.44 pKi 3630.78 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151 B 5.65 pKi 2250 nM Ki J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL Inhibition of human dopamine D2 receptor B 5.65 pKi 2230 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
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 7.44 pKi 36.1 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity on human Dopamine receptor D3 expressed in CHO cells using radioligand [3H]-YM 09151 B 5.1 pKi >8000 nM Ki J Med Chem (1997) 40: 1-3 [PMID:9016321]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 8.3 pKd 5 nM Kd J Pharmacol Exp Ther (1997) 282: 1020-7 [PMID:9262371]
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 8.37 pKi 4.29 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151 B 8.42 pKi 3.8 nM Ki J Med Chem (1997) 40: 1-3 [PMID:9016321]
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 8.44 pKi 3.63 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Binding affinity towards human dopamine receptor D4 B 8.44 pKi 3.6 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]

ChEMBL data shown on this page come from version 36:

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]