Mutant Browser

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Protein name Generic number Position Segment Mutation FoldChange or Qual Exp Type Ligand Reference Review
5ht6r_human 3.32x32 106 TM3 D => A 1.0 pK(i) (Binding - Radioligand competition/displacement) LANDIPIRDINE Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.36x36 110 TM3 C => A 1.995↑ pK(i) (Binding - Radioligand competition/displacement) LANDIPIRDINE Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.43x44 193 TM5 S => A 2.513↓ pK(i) (Binding - Radioligand competition/displacement) LANDIPIRDINE Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.46x461 196 TM5 T => A 2.512↑ pK(i) (Binding - Radioligand competition/displacement) LANDIPIRDINE Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.48x48 281 TM6 W => A 25.0↓ pK(i) (Binding - Radioligand competition/displacement) LANDIPIRDINE Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.51x51 284 TM6 F => A 31.25↓ pK(i) (Binding - Radioligand competition/displacement) LANDIPIRDINE Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.55x55 288 TM6 N => A 3.165↓ pK(i) (Binding - Radioligand competition/displacement) LANDIPIRDINE Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.32x32 106 TM3 D => A 5.0↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085037 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.36x36 110 TM3 C => A 2.512↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085037 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.43x44 193 TM5 S => A 1.259↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085037 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.46x461 196 TM5 T => A 3.162↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085037 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.48x48 281 TM6 W => A 3.165↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085037 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.51x51 284 TM6 F => A 5.0↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085037 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.55x55 288 TM6 N => A 1.585↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085037 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.32x32 106 TM3 D => A 31.25↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085617 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.36x36 110 TM3 C => A 2.512↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085617 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.43x44 193 TM5 S => A N/A pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085617 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.46x461 196 TM5 T => A 2.512↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085617 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.48x48 281 TM6 W => A 7.937↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085617 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.51x51 284 TM6 F => A 50.0↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085617 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.55x55 288 TM6 N => A 5.0↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1085617 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.32x32 106 TM3 D => A 12.658↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1086326 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.36x36 110 TM3 C => A 1.995↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1086326 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.43x44 193 TM5 S => A 1.259↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1086326 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.46x461 196 TM5 T => A 1.585↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1086326 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.48x48 281 TM6 W => A 100.0↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1086326 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.51x51 284 TM6 F => A 15.873↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1086326 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.55x55 288 TM6 N => A 5.0↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1086326 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.34x34 267 TM6 S => K 2.5↑ K(d) (Binding - Radioligand saturation) 5-hydroxytryptamine Purohit A et al (2003) Vass M et al (2019)
5ht6r_human 6.34x34 267 TM6 S => K 10.0↑ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Purohit A et al (2003) Vass M et al (2019)
5ht6r_human 6.34x34 267 TM6 S => K 1.035↓ K(d) (Binding - Radioligand saturation) LSD Purohit A et al (2003) Vass M et al (2019)
5ht6r_human 6.48x48 281 TM6 W => A 2.344↑ K(i) (Binding - Radioligand competition/displacement) SB258585 de la Fuente T et al (2010) Vass M et al (2019)
5ht6r_human 6.52x52 285 TM6 F => A 142.857↓ K(i) (Binding - Radioligand competition/displacement) SB258585 de la Fuente T et al (2010) Vass M et al (2019)
5ht6r_human 6.55x55 288 TM6 N => A 35.714↓ K(i) (Binding - Radioligand competition/displacement) SB258585 de la Fuente T et al (2010) Vass M et al (2019)
5ht6r_human 3.32x32 106 TM3 D => A 1.585↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1082777 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.36x36 110 TM3 C => A 2.512↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1082777 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.43x44 193 TM5 S => A 2.513↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1082777 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 5.46x461 196 TM5 T => A 2.512↑ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1082777 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.48x48 281 TM6 W => A 100.0↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1082777 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.51x51 284 TM6 F => A 31.25↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1082777 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 6.55x55 288 TM6 N => A 2.513↓ pK(i) (Binding - Radioligand competition/displacement) CHEMBL1082777 Harris RN 3rd et al (2010) Vass M et al (2019)
5ht6r_human 3.36x36 110 TM3 C => A 10.0↓ pIC50 (Functional - cAMP accumulation) CHEMBL5220504 Gonzalez-Vera JA et al (2017)
5ht6r_human 5.43x44 193 TM5 S => A 76.923↓ pIC50 (Functional - cAMP accumulation) CHEMBL5220504 Gonzalez-Vera JA et al (2017)
5ht6r_human 6.52x52 285 TM6 F => A 1000.0↓ pIC50 (Functional - cAMP accumulation) CHEMBL5220504 Gonzalez-Vera JA et al (2017)
5ht6r_human 6.55x55 288 TM6 N => A 7.937↓ pIC50 (Functional - cAMP accumulation) CHEMBL5220504 Gonzalez-Vera JA et al (2017)
5ht6r_human 3.36x36 110 TM3 C => A 3.165↓ pEC50 (Functional - cAMP accumulation) 5-hydroxytryptamine Gonzalez-Vera JA et al (2017)
5ht6r_human 5.43x44 193 TM5 S => A 76.923↓ pEC50 (Functional - cAMP accumulation) 5-hydroxytryptamine Gonzalez-Vera JA et al (2017)
5ht6r_human 6.52x52 285 TM6 F => A 250.0↓ pEC50 (Functional - cAMP accumulation) 5-hydroxytryptamine Gonzalez-Vera JA et al (2017)
5ht6r_human 6.55x55 288 TM6 N => A 3.165↓ pEC50 (Functional - cAMP accumulation) 5-hydroxytryptamine Gonzalez-Vera JA et al (2017)
5ht6r_human 3.32x32 106 TM3 D => A Abolished pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 3.36x36 110 TM3 C => A 500.0↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 3.37x37 111 TM3 S => A 100.0↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 3.37x37 111 TM3 S => T N/A pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 45.52x52 182 ECL2 L => A 30.303↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 5.39x40 189 TM5 V => A 8.547↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 5.42x43 192 TM5 A => Y Abolished pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 6.48x48 281 TM6 W => A N/A pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 6.51x51 284 TM6 F => A N/A pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 6.52x52 285 TM6 F => A 500.0↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 6.55x55 288 TM6 N => A 5.495↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 6.55x55 288 TM6 N => S 1.0 pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 7.43x42 310 TM7 Y => A 166.667↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht6r_human 3.33x33 107 TM3 V => A 1.0 pEC50 (Functional - cAMP accumulation) CHEMBL365751 Pei Y et al (2023)
5ht6r_human 3.37x37 111 TM3 S => A 1.0 pEC50 (Functional - cAMP accumulation) CHEMBL365751 Pei Y et al (2023)
5ht6r_human 5.38x39 188 TM5 F => A 40.0↓ pEC50 (Functional - cAMP accumulation) CHEMBL365751 Pei Y et al (2023)
5ht6r_human 6.48x48 281 TM6 W => A Abolished pEC50 (Functional - cAMP accumulation) CHEMBL365751 Pei Y et al (2023)
5ht6r_human 6.51x51 284 TM6 F => A 3.984↓ pEC50 (Functional - cAMP accumulation) CHEMBL365751 Pei Y et al (2023)
5ht6r_human 7.43x42 310 TM7 Y => A 40.0↓ pEC50 (Functional - cAMP accumulation) CHEMBL365751 Pei Y et al (2023)
Protein name Generic number Segment Position Mutation FoldChange or Qual Exp Type Ligand Reference Review


Residue

Diagrams

ICL1 P A L R ICL1ECL1 R W V L ECL1ICL2 P L R Y K L R M ICL2ECL2 W H E L G H A R P P V P G Q C R L L A ECL2ICL3 T G M A S Q A S E T L Q V P R T P R P G V E S A D S R R L A ICL3ECL3 D C I ECL3N-term M V P E P G P T A N S T P A W G A G P P S A P G G N-termC-term P R C P R E R Q A S L A S P S L R T S H S G P R P G L S L Q Q V L P L P L P P D S D S D S D A G S G G S S G L R L T A Q L L L P G E A T Q D P P L P T R A A A A V N F F N I D P A E P E L R P H P L G I P T N C-term S G W V A A A L C V V I A L T A A A N S L L I A L I C T Q N T S N F F L V S L F T S D L M V G L V V M P P A M L N A L Y G A R G L C L L W T A F D V M C C S A S I L N L C L I S L D R Y L L I L S T P L R A L A L V L G A W S L A A L A S F L P L L L G S L P F V L V A S G L T F F L P S G A I C F T Y C R I L L A A R K Q A V Q V A S L T T K H S R K A L K A S L T L G I L L G M F F V T W L P F F V A N I V Q A V C S P G L F D V L T W L G Y C N S T M N P I I Y P L F M R D L G R F K R A F L P C
Download: PNG | SVG Increased binding/potency: >5-fold, >10-fold; Reduced binding/potency: >5-fold, >10-fold; No/low effect (<5-fold); and N/A
S N A A A T L A I V V C L A A A V W G S 1 V S L F T S D L M V G V L V M P P A M L N 2 L C L N L I S A S C C M V D F A T W L L 3 A L A L V L G A W S L A A L A S F L P L 4 Y T F C I A G S P L F F T L G S A V L V F 5 G I L L G M F F V T W L P F F V A N I V 6 I P N M T S N C Y G L W T L V D F L G 7
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Residue Table


GPCRdb(A)
GPCRdb(A)
5-HT6 receptor
TM3
3x32 3.32x32 D106
3x33 3.33x33 V107
3x36 3.36x36 C110
3x37 3.37x37 S111
TM5
5x39 5.38x39 F188
5x40 5.39x40 V189
5x43 5.42x43 A192
5x44 5.43x44 S193
5x461 5.46x461 T196
TM6
6x34 6.34x34 S267
6x48 6.48x48 W281
6x51 6.51x51 F284
6x52 6.52x52 F285
6x55 6.55x55 N288
TM7
7x42 7.43x42 Y310