General Information of the Protein
Protein ID
PT02458
Protein Name
5-hydroxytryptamine receptor 1F
Secondarily
Protein Name
Serotonin receptor 1F
Gene Name
HTR1F
Secondarily
Gene Name
HTR1EL
Sequence
MDFLNSSDQNLTSEELLNRMPSKILVSLTLSGLALMTTTINSLVIAAIIVTRKLHHPANYLICSLAVTDFLVAVLVMPFSIVYIVRESWIMGQVVCDIWLSVDITCCTCSILHLSAIALDRYRAITDAVEYARKRTPKHAGIMITIVWIISVFISMPPLFWRHQGTSRDDECIIKHDHIVSTIYSTFGAFYIPLALILILYYKIYRAAKTLYHKRQASRIAKEEVNGQVLLESGEKSTKSVSTSYVLEKSLSDPSTDFDKIHSTVRSLRSEFKHEKSWRRQKISGTRERKAATTLGLILGAFVICWLPFFVKELVVNVCDKCKISEEMSNFLAWLGYLNSLINPLIYTIFNEDFKKAFQKLVRCRC
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Serotonin receptor
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
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Uniprot ID
P30939
Ensembl ID
ENSG00000179097
HGNC ID
HGNC:5292
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0395135
 Compound Info 
(R)-2-(4-Fluoro-phenyl)-2-{1-[3-(5-[1,2,4]triazol-4-yl-1H-indol-3-yl)-propyl]-piperidin-4-ylamino}-ethanol
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C26H31FN6O
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0860616
 Compound Info 
3-Chloro-N-[3-((R)-1-methyl-pyrrolidin-2-ylmethyl)-1H-indol-5-yl]-benzenesulfonamide
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C20H22ClN3O2S
  1
1
Ki = 2.7 nM
 Bioactivity Info 
   TI
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CP0330654
 Compound Info 
2-[1-(benzenesulfonyl)indol-4-yl]-N,N-dimethylethanamine
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C18H20N2O2S
  1
1
Ki = 3.9 nM
 Bioactivity Info 
   TI
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CP0853639
 Compound Info 
2-Chloro-N-(3-(R)-1-pyrrolidin-2-ylmethyl-1H-indol-5-yl)-benzenesulfonamide
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C19H20ClN3O2S
  1
1
Ki = 12.3 nM
 Bioactivity Info 
   TI
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CP0873359
 Compound Info 
2-Chloro-N-[3-((R)-1-methyl-pyrrolidin-2-ylmethyl)-1H-indol-5-yl]-benzenesulfonamide
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C20H22ClN3O2S
  1
1
Ki = 16 nM
 Bioactivity Info 
   TI
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CP0777252
 Compound Info 
2-Iodo-N-(3-(R)-1-pyrrolidin-2-ylmethyl-1H-indol-5-yl)-benzenesulfonamide
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C20H22IN3O2S
  1
1
Ki = 17.8 nM
 Bioactivity Info 
   TI
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CP0379189
 Compound Info 
2-(1-Benzenesulfonyl-1H-indol-4-yl)-ethylamine
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C16H16N2O2S
  1
1
Ki = 47 nM
 Bioactivity Info 
   TI
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CP0165719
 Compound Info 
N-[3-[(8aR)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-4-methoxyphenyl]-5-chloro-3-methyl-1-benzothiophene-2-sulfonamide
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C23H26ClN3O3S2
  1
1
Ki = 199.53 nM
 Bioactivity Info 
   TI
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CP0113176
 Compound Info 
5-Chloro-3-methyl-benzo[b]thiophene-2-sulfonic acid [4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide
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C21H24ClN3O3S2
  1
1
Ki = 251.19 nM
 Bioactivity Info 
   TI
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CP0185590
 Compound Info 
4-Bromo-N-[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-benzenesulfonamide
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C18H22BrN3O3S
  1
1
Ki = 316.23 nM
 Bioactivity Info 
   TI
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CP0183577
 Compound Info 
5-Chloro-3-methyl-benzo[b]thiophene-2-sulfonic acid ((S)-3-hexahydro-pyrrolo[1,2-a]pyrazin-2-yl-4-methoxy-phenyl)-amide
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C23H26ClN3O3S2
  1
1
Ki = 316.23 nM
 Bioactivity Info 
   TI
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CP0418991
 Compound Info 
[1-(benzenesulfonyl)-4-[2-(dimethylamino)ethyl]indol-2-yl]-phenylmethanone
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C25H24N2O3S
  1
1
Ki = 570 nM
 Bioactivity Info 
   TI
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CP0255950
 Compound Info 
2-[1-(benzenesulfonyl)indol-3-yl]-N,N-dimethylethanamine
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C18H20N2O2S
  1
1
Ki = 770 nM
 Bioactivity Info 
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CP0318039
 Compound Info 
3-(2-Dimethylamino-ethyl)-1H-indole-2-carboxylic acid ethyl ester
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C15H20N2O2
  1
1
Ki = 2000 nM
 Bioactivity Info 
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CP0045069
 Compound Info 
2-[1-(benzenesulfonyl)-5-methoxyindol-3-yl]-N,N-dimethylethanamine
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C19H22N2O3S
  1
1
Ki = 2500 nM
 Bioactivity Info 
   TI
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CP0674190
 Compound Info 
5-Chloro-3-methyl-benzo[b]thiophene-2-sulfonic acid (4-methoxy-3-piperazin-1-yl-phenyl)-amide hydrochloride
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C20H23Cl2N3O3S2
  1
1
Ki < 1000 nM
 Bioactivity Info 
   TI
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CP0041243
 Compound Info 
5-chloro-N-[4-methoxy-3-(piperazin-1-yl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamide hydrochloride
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C20H22ClN3O3S2
  1
1
Ki < 1000 nM
 Bioactivity Info 
   TI
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CP0216543
 Compound Info 
N-[3-(1,3,4,6,7,8,9,9a-octahydropyrido[1,2-a]pyrazin-2-yl)-4-methoxyphenyl]-5-chloro-3-methyl-1-benzothiophene-2-sulfonamide
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C24H28ClN3O3S2
  1
1
Ki < 1000 nM
 Bioactivity Info 
   TI
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CP0096286
 Compound Info 
(R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidin-1-ylsulfonyl)phenol
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C18H28N2O3S
  1
1
Ki < 3162.28 nM
 Bioactivity Info 
   TI
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CP0271460
 Compound Info 
(R)-1-(2-(1-(3,4-Dichloro-benzene sulfonyl)-pyrrolidin-2-yl)-ethyl)-4-methyl piperidine
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C18H26Cl2N2O2S
  1
1
Ki < 3162.28 nM
 Bioactivity Info 
   TI
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CP0051242
 Compound Info 
(R)-1-(2-(1-(3-bromo-benzenesulfonyl)-pyrrolidin-2-yl)-ethyl)-4-methyl piperidine
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C18H27BrN2O2S
  1
1
Ki < 5011.87 nM
 Bioactivity Info 
   TI
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CP0156235
 Compound Info 
3,N-Dimethyl-N-[(R)-1-methyl-3-(4-methyl-piperidin-1-yl)-propyl]-benzenesulfonamide
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C18H30N2O2S
  1
1
Ki < 6309.57 nM
 Bioactivity Info 
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CP0198069
 Compound Info 
(R)-4-Methyl-1-(2-(1-(naphthalene-1-sulfonyl)-pyrrolidin-2-yl)-ethyl)-piperidine(10)
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C22H30N2O2S
  1
1
Ki < 10000 nM
 Bioactivity Info 
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CP0712961
 Compound Info 
(R)-sulfonamide1-(4-methylhexahydro-1-pyridinyl)-2-[1-(1-naphthylsulfonyl)hexahydro-2-pyridinyl]ethane
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C23H32N2O2S
  1
1
Ki < 10000 nM
 Bioactivity Info 
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CP0182705
 Compound Info 
(R)-4-Methyl-1-(2-(1-toluene-3-sulfonyl)-pyrrolidin-2-yl)-ethyl)-piperidine (Oxalate salt)
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C19H30N2O2S
  1
1
Ki < 10000 nM
 Bioactivity Info 
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CP0658944
 Compound Info 
(RS)-1-(4-methylhexahydro-1-pyridinyl)-2-[1-(1-naphthylsulfonyl)hexahydro-2-pyridinyl]ethane
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C23H32N2O2S
  1
1
Ki < 10000 nM
 Bioactivity Info 
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0138764
 Compound Info 
2,4,6-trifluoro-N-[6-[fluoro-(1-methylpiperidin-4-ylidene)methyl]pyridin-2-yl]benzamide
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C19H17F4N3O
  1
1 IC50 = 0.32 nM
CP0357652
 Compound Info 
COL-144
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C19H18F3N3O2
  1
1 Ki = 2.21 nM
CP0239322
 Compound Info 
2,4,6-Trifluoro-N-[3-(1-methyl-piperidin-4-yl)-furo[3,2-b]pyridin-5-yl]-benzamide
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C20H18F3N3O2
  1
1 Ki = 2.3 nM
CP0047688
 Compound Info 
2-Chloro-6-fluoro-N-[3-(1-methyl-piperidin-4-yl)-furo[3,2-b]pyridin-5-yl]-benzamide
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C20H19ClFN3O2
  1
1 Ki = 2.9 nM
CP0343107
 Compound Info 
2-Chloro-4-fluoro-N-[3-(1-methyl-piperidin-4-yl)-furo[3,2-b]pyridin-5-yl]-benzamide
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C20H19ClFN3O2
  1
1 Ki = 3 nM
CP0331815
 Compound Info 
4-Fluoro-N-[3-(1-methyl-piperidin-4-yl)-furo[3,2-b]pyridin-5-yl]-benzamide
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C20H20FN3O2
  1
1 Ki = 3.1 nM
CP0184375
 Compound Info 
2-Chloro-4-fluoro-N-[3-(1-methyl-piperidin-4-yl)-benzo[d]isoxazol-5-yl]-benzamide
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C20H19ClFN3O2
  1
1 Ki = 3.6 nM
CP0126097
 Compound Info 
4-fluoro-N-[3-(1-methylpiperidine-4-carbonyl)phenyl]benzamide
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C20H21FN2O2
  1
1 Ki = 5.1 nM
CP0220348
 Compound Info 
4-fluoro-N-[2-fluoro-3-(1-methylpiperidine-4-carbonyl)phenyl]benzamide
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C20H20F2N2O2
  1
1 Ki = 8.3 nM
CP0126388
 Compound Info 
4-fluoro-N-[6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl]benzamide
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C19H20FN3O2
  1
1 Ki = 9.5 nM
CP0306223
 Compound Info 
2,4-Difluoro-N-[3-(1-methyl-piperidin-4-yl)-benzo[d]isoxazol-5-yl]-benzamide
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C20H19F2N3O2
  1
1 Ki = 12 nM
CP0050773
 Compound Info 
2-Chloro-4-fluoro-N-[3-(1-methyl-piperidin-4-yl)-2,3-dihydro-1H-benzoimidazol-5-yl]-benzamide
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C20H22ClFN4O
  1
1 Ki = 13 nM
CP0310030
 Compound Info 
2,4,6-Trifluoro-N-[3-(1-methyl-piperidin-4-yl)-2,3-dihydro-1H-benzoimidazol-5-yl]-benzamide
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C20H21F3N4O
  1
1 Ki = 17 nM
Clinical Information about the Protein
Target 1 ( 5-HT 1F receptor (HTR1F) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Migraine [ICD-11: 8A80]
2 Hyperprolactinaemia [ICD-11: 5A60.1]
Approved Drug(s) 2 Approved Drugs  2
1 Lasmiditan
 Drug Info 
Approved
Migraine
2 Metergolin
 Drug Info 
Approved
Hyperprolactinaemia
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 LY-334370
 Drug Info 
Phase 2
Migraine
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01005 D(2) dopamine receptor Homo sapiens, Human
 Protein Info 
PT01734 D(2) dopamine receptor Bos taurus, Bovine
 Protein Info