General Information of the Protein
Protein ID
PT00827
Protein Name
5-hydroxytryptamine receptor 1D
Secondarily
Protein Name
Serotonin 1D alpha receptor
Serotonin receptor 1D
Gene Name
HTR1D
Secondarily
Gene Name
HTR1DA
HTRL
Sequence
MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVLTTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDITCCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAKAQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFTTAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKATKILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFNEEFRQAFQKIVPFRKAS
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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 ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other 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. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction.
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Uniprot ID
P28221
HGNC ID
HGNC:5289
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: CL000026 , CHO-K1
Compound ID Compound Name Compound Formula
CP0056131
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-[4-(3-methoxy-phenyl)-piperazin-1-yl]-ethanone
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C23H28N4O3
 1
1
EC50 = 0.24 nM
   TI
   LI
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   TS
CP0162751
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-phenyl-piperazin-1-yl)-ethanone
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C22H26N4O2
 1
1
EC50 = 0.45 nM
   TI
   LI
   LO
   TS
CP0102236
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-o-tolyl-piperazin-1-yl)-ethanone
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C23H28N4O2
 1
1
EC50 = 0.6 nM
   TI
   LI
   LO
   TS
CP0151604
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-naphthalen-1-yl-piperazin-1-yl)-ethanone
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C26H28N4O2
 1
1
EC50 = 2.8 nM
   TI
   LI
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   TS
CP0005653
(3-[2-(dimethylamino)ethyl]-1H-indol-5-yl)-N-methylmethanesulfonamide
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C14H21N3O2S
 5
1
EC50 = 30 nM
   TI
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2
IC50 = 2.951 nM
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3
Ki = 1.2 nM
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4
Ki = 5.7 nM
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5
Ki = 8.5 nM
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CP0010235
2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine
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C19H30N2O
 1
1
EC50 = 68 nM
   TI
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CP0048312
3-(4-{7-[4-(5-carbamoyl-1H-3-indolyl)-3-cyclohexenylamino]heptylamino}-1-cyclohexenyl)-1H-5-indolecarboxamide
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C37H46N6O2
 1
1
IC50 = 0.05 nM
   TI
   LI
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CP0136962
3-(3-{4-[2-(3-Fluoro-phenyl)-ethyl]-piperazin-1-yl}-propyl)-5-[1,2,4]triazol-4-yl-1H-indole
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C25H29FN6
 1
1
IC50 = 0.6 nM
   TI
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CP0099897
(S)-4-((3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one
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C16H21N3O2
 1
1
IC50 = 2.818 nM
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CP0454849
4-[[3-(3-aminocyclobutyl)-1H-indol-5-yl]methyl]-1,3-oxazolidin-2-one
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C16H19N3O2
 1
1
IC50 = 3.631 nM
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CP0463655
4-[[3-[3-(methylamino)cyclobutyl]-1H-indol-5-yl]methyl]-1,3-oxazolidin-2-one
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C17H21N3O2
 1
1
IC50 = 7.079 nM
   TI
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CP0449000
CP 122288
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C16H23N3O2S
 1
1
IC50 = 7.244 nM
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CP0460129
3-(5-phenoxy-1H-indol-3-yl)cyclobutan-1-amine
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C18H18N2O
 1
1
IC50 = 14.45 nM
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   LI
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CP0454850
3-[3-(dimethylamino)cyclobutyl]-1H-indole-5-carboxamide
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C15H19N3O
 1
1
IC50 = 14.79 nM
   TI
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CP0532404
(4S)-4-[[3-[[3-(dimethylamino)cyclobutyl]methyl]-1H-indol-5-yl]methyl]-1,3-oxazolidin-2-one
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C19H25N3O2
 1
1
IC50 = 28.84 nM
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CP0463786
N,N-dimethyl-3-(5-phenoxy-1H-indol-3-yl)cyclobutan-1-amine
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C20H22N2O
 1
1
IC50 = 64.57 nM
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CP0466096
N,N-dimethyl-2-(5-phenylmethoxy-1H-indol-3-yl)ethanamine
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C19H22N2O
 1
1
IC50 = 76 nM
   TI
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CP0421471
3-(2-Diethylamino-ethyl)-1H-indol-5-ol
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C14H20N2O
 1
1
IC50 = 77 nM
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CP0421474
N,N-diethyl-2-(5-phenylmethoxy-1H-indol-3-yl)ethanamine
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C21H26N2O
 1
1
IC50 = 110 nM
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CP0374352
N-benzyl-3-[3-(dimethylamino)cyclobutyl]-1H-indole-5-carboxamide
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C22H25N3O
 1
1
IC50 = 141.25 nM
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CP0438598
1-[3-[3-(dimethylamino)cyclobutyl]-1H-indol-5-yl]-N-methylmethanesulfonamide
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C16H23N3O2S
 1
1
IC50 = 190.55 nM
   TI
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CP0508686
2-[2-[3-[3-(dimethylamino)cyclobutyl]-1H-indol-5-yl]ethyl]isoindole-1,3-dione
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C24H25N3O2
 1
1
IC50 = 194.98 nM
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CP0382996
N-benzyl-2-[3-[3-(dimethylamino)cyclobutyl]-1H-indol-5-yl]acetamide
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C23H27N3O
 1
1
IC50 = 338.84 nM
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CP0481162
N-[2-(5-phenylmethoxy-1H-indol-3-yl)ethyl]-N-propylpropan-1-amine
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C23H30N2O
 1
1
IC50 = 470 nM
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CP0502412
3-[2-[3-(3-aminocyclobutyl)-1H-indol-5-yl]ethyl]-5,5-dimethylimidazolidine-2,4-dione
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C19H24N4O2
 1
1
IC50 = 501.19 nM
   TI
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CP0382933
N,N-dimethyl-3-[5-(3-methyl-1,2,4-oxadiazol-5-yl)-1H-indol-3-yl]cyclobutan-1-amine
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C17H20N4O
 1
1
IC50 = 562.34 nM
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CP0456955
2-[3-[3-(dimethylamino)cyclobutyl]-1H-indol-5-yl]acetamide
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C16H21N3O
 1
1
IC50 = 724.44 nM
   TI
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CP0133551
3-(2-Dipropylamino-ethyl)-1H-indol-5-ol
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C16H24N2O
 1
1
IC50 = 820 nM
   TI
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CP0528891
N,N-dimethyl-3-[5-[(3-methyl-1,2,4-oxadiazol-5-yl)methyl]-1H-indol-3-yl]cyclobutan-1-amine
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C18H22N4O
 1
1
IC50 = 933.25 nM
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CP0422303
3-[2-[3-[3-(dimethylamino)cyclobutyl]-1H-indol-5-yl]ethyl]-5,5-dimethylimidazolidine-2,4-dione
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C21H28N4O2
 1
1
IC50 = 1479.11 nM
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CP0460915
N,N-dimethyl-3-[5-[(5-methyl-1H-1,2,4-triazol-3-yl)methyl]-1H-indol-3-yl]cyclobutan-1-amine
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C18H23N5
 1
1
IC50 = 2041.74 nM
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CP0463326
3-[[3-[3-(dimethylamino)cyclobutyl]-1H-indol-5-yl]methyl]imidazolidine-2,4-dione
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C18H22N4O2
 1
1
IC50 = 2454.71 nM
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CP0502478
3-[[3-[3-(dimethylamino)cyclobutyl]-1H-indol-5-yl]methyl]-5,5-dimethylimidazolidine-2,4-dione
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C20H26N4O2
 1
1
IC50 = 3090.3 nM
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CP0479795
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-N-[4-(4-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-acetyl}-piperazin-1-yl)-phenyl]-acetamide
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C34H39N7O4
 1
1
Ki = 0.09 nM
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CP0234879
2-(5-((4-((3-(2-aminoethyl)-1H-indol-5-yloxy)methyl)phenyl)methoxy)-1H-indol-3-yl)ethanamine
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C28H30N4O2
 1
1
Ki = 0.11 nM
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CP0436395
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-N-(4-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-acetylamino}-phenyl)-acetamide
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C30H32N6O4
 1
1
Ki = 0.11 nM
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CP0394213
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-ethyl}-piperazin-1-yl)-ethanone
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C28H36N6O3
 1
1
Ki = 0.16 nM
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CP0492326
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-N-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-ethyl}-acetamide
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C24H29N5O3
 1
1
Ki = 0.18 nM
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CP0403765
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(1'-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-acetyl}-[4,4']bipiperidinyl-1-yl)-ethanone
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C34H44N6O4
 1
1
Ki = 0.27 nM
   TI
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CP0190867
(E)-3-[3-(2-Dimethylamino-ethyl)-1H-indol-5-yl]-N-(4-methoxy-benzyl)-acrylamide
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C23H27N3O2
 1
1
Ki = 0.3 nM
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CP0441180
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-N-(3-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-acetylamino}-propyl)-acetamide
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C27H34N6O4
 1
1
Ki = 0.3 nM
   TI
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CP0070886
4-fluoro-N-(3-{1-[7-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)heptyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
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C47H52F2N6O2
 1
1
Ki = 0.3 nM
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CP0446193
2-(5-{3-[3-(2-Amino-ethyl)-1H-indol-5-yloxymethyl]-benzyloxy}-1H-indol-3-yl)-ethylamine
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C28H30N4O2
 1
1
Ki = 0.35 nM
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CP0449404
2-{5-[2-(4-{2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-ethyl}-piperazin-1-yl)-ethoxy]-1H-indol-3-yl}-ethylamine
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C28H38N6O2
 1
1
Ki = 0.35 nM
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CP0418821
1,3-Bis-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-ethyl}-urea
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C25H32N6O3
 1
1
Ki = 0.4 nM
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CP0106415
2-(5-(2-(8-(4-methylpiperazin-1-yl)naphthalen-2-yloxy)ethoxy)-1H-indol-3-yl)ethanamine
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C27H32N4O2
 1
1
Ki = 0.4 nM
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CP0394215
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-{2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-acetyl}-piperazin-1-yl)-ethanone
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C28H34N6O4
 1
1
Ki = 0.42 nM
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CP0372361
Biphenyl-4,4'-disulfonic acid bis-({6-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-hexyl}-amide)
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C44H56N6O6S2
 1
1
Ki = 0.45 nM
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CP0460901
2-(5-{6-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-hexyloxy}-1H-indol-3-yl)-ethylamine
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C26H34N4O2
 1
1
Ki = 0.46 nM
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CP0001238
14C-5-hydroxy tryptamine creatinine disulfate
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C10H12N2O
 2
1
Ki = 0.5 nM
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2
Ki = 5.06 nM
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CP0435734
4-fluoro-N-(3-{1-[6-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)hexyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
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C46H50F2N6O2
 1
1
Ki = 0.6 nM
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CP0169227
C-[3-(2-Dimethylamino-ethyl)-1H-indol-5-yl]-N-[4-({[3-(2-dimethylamino-ethyl)-1H-indol-5-ylmethanesulfonyl]-methyl-amino}-methyl)-benzyl]-N-methyl-methanesulfonamide
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C36H48N6O4S2
 1
1
Ki = 0.89 nM
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CP0388169
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]undecanediamide
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C39H54N6O2
 1
1
Ki = 0.9 nM
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CP0439237
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]octanediamide
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C36H48N6O2
 1
1
Ki = 0.9 nM
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CP0446013
(S)-1-(2-(4-(4-methoxyphenyl)piperazin-1-yl)ethyl)-N-methyl-3,4-dihydro-1H-isochromene-6-carboxamide
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C24H31N3O3
 1
1
Ki = 0.9 nM
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CP0422477
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]pentanediamide
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C33H42N6O2
 1
1
Ki = 0.95 nM
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CP0474372
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]decanediamide
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C38H52N6O2
 1
1
Ki = 0.95 nM
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CP0446075
2-(5-{2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-ethoxy}-1H-indol-3-yl)-ethylamine
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C22H26N4O2
 1
1
Ki = 1 nM
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CP0493405
4-fluoro-N-(3-{1-[9-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)nonyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
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C49H56F2N6O2
 1
1
Ki = 1 nM
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CP0473794
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]tridecanediamide
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C41H58N6O2
 1
1
Ki = 1.4 nM
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CP0403731
2-(5-{2-[3-(2-Amino-ethyl)-1H-indol-5-yloxymethyl]-benzyloxy}-1H-indol-3-yl)-ethylamine
   Show/Hide
C28H30N4O2
 1
1
Ki = 1.5 nM
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CP0435738
4-fluoro-N-{3-[1-(2-{2-[2-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)ethoxy]ethoxy}ethyl)piperidin-4-yl]-1H-indol-5-yl}benzamide
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C46H50F2N6O4
 1
1
Ki = 1.5 nM
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CP0275909
N-[4-[4-[2-[[3-(2-aminoethyl)-1H-indol-5-yl]oxy]acetyl]piperazin-1-yl]phenyl]acetamide
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C24H29N5O3
 1
1
Ki = 1.7 nM
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CP0439236
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]tetradecanediamide
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C42H60N6O2
 1
1
Ki = 1.7 nM
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CP0493409
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]pentadecanediamide
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C43H62N6O2
 1
1
Ki = 2.3 nM
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CP0135602
[3-(2-aminoethyl)-1H-indol-5-yl] trifluoromethanesulfonate
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C11H11F3N2O3S
 1
1
Ki = 2.8 nM
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CP0196504
[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl] trifluoromethanesulfonate
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C13H15F3N2O3S
 1
1
Ki = 3.2 nM
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CP0455102
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]propanediamide
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C31H38N6O2
 1
1
Ki = 3.4 nM
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CP0497725
4-fluoro-N-(3-{1-[2-(2-{2-[2-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)ethoxy]ethoxy}ethoxy)ethyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
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C48H54F2N6O5
 1
1
Ki = 3.9 nM
   TI
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CP0393093
(R)-8-Dipropylamino-4-fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
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C19H25FN2O
 1
1
Ki = 4.4 nM
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CP0497437
8-Dipropylamino-4-fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
   Show/Hide
C19H25FN2O
 1
1
Ki = 4.6 nM
   TI
   LI
   LO
   TS
CP0065057
(R)-8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbonitrile
   Show/Hide
C19H25N3
 1
1
Ki = 6.7 nM
   TI
   LI
   LO
   TS
CP0043151
8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbonitrile
   Show/Hide
C19H25N3
 1
1
Ki = 7.5 nM
   TI
   LI
   LO
   TS
CP0500731
(4-Fluoro-1-propyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C21H31FN2
 1
1
Ki = 8.4 nM
   TI
   LI
   LO
   TS
CP0393274
8-Dipropylamino-4-fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbonitrile
   Show/Hide
C19H24FN3
 1
1
Ki = 8.6 nM
   TI
   LI
   LO
   TS
CP0393208
(4-Fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C18H25FN2
 1
1
Ki = 11 nM
   TI
   LI
   LO
   TS
CP0457588
N,N'-bis[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]hexadecanediamide
   Show/Hide
C44H64N6O2
 1
1
Ki = 11.3 nM
   TI
   LI
   LO
   TS
CP0332330
[3-[2-(diethylamino)ethyl]-1H-indol-5-yl] trifluoromethanesulfonate
   Show/Hide
C15H19F3N2O3S
 1
1
Ki = 12 nM
   TI
   LI
   LO
   TS
CP0422474
4-fluoro-N-(3-{1-[12-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)dodecyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
   Show/Hide
C52H62F2N6O2
 1
1
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0467895
4-fluoro-N-(3-{1-[11-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)undecyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
   Show/Hide
C51H60F2N6O2
 1
1
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0497724
4-fluoro-N-(3-{1-[10-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)decyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
   Show/Hide
C50H58F2N6O2
 1
1
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0492002
((R)-4-Fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C18H25FN2
 1
1
Ki = 14 nM
   TI
   LI
   LO
   TS
CP0056626
(8R)-N,N-dipropyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-amine
   Show/Hide
C18H26N2
 1
1
Ki = 16 nM
   TI
   LI
   LO
   TS
CP0384127
(1-Methylsulfanyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C19H28N2S
 1
1
Ki = 18 nM
   TI
   LI
   LO
   TS
CP0348071
(1-Chloro-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C18H25ClN2
 1
1
Ki = 23 nM
   TI
   LI
   LO
   TS
CP0457582
4-fluoro-N-(3-{1-[(2E)-4-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)but-2-en-1-yl]piperidin-4-yl}-1H-indol-5-yl)benzamide
   Show/Hide
C44H44F2N6O2
 1
1
Ki = 24 nM
   TI
   LI
   LO
   TS
CP0378932
8-Dipropylamino-1,3,6,7,8,9-hexahydro-benzo[e]indol-2-one
   Show/Hide
C18H26N2O
 1
1
Ki = 26 nM
   TI
   LI
   LO
   TS
CP0276816
(R)-8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
   Show/Hide
C19H26N2O
 1
1
Ki = 31 nM
   TI
   LI
   LO
   TS
CP0425321
(S)-8-Dipropylamino-4-fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
   Show/Hide
C19H25FN2O
 1
1
Ki = 34 nM
   TI
   LI
   LO
   TS
CP0503251
1-(8-Dipropylamino-4-fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indol-1-yl)-propan-1-one
   Show/Hide
C21H29FN2O
 1
1
Ki = 36 nM
   TI
   LI
   LO
   TS
CP0467899
5-amino-3-(N-methylpiperidin-4-yl)-1H-indole
   Show/Hide
C14H19N3
 1
1
Ki = 39.6 nM
   TI
   LI
   LO
   TS
CP0258010
(+/-)-Dipropyl-(6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-amine
   Show/Hide
C18H26N2
 1
1
Ki = 40 nM
   TI
   LI
   LO
   TS
CP0099933
(S)-8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbonitrile
   Show/Hide
C19H25N3
 1
1
Ki = 42 nM
   TI
   LI
   LO
   TS
CP0373268
(1-Methyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C19H28N2
 1
1
Ki = 43 nM
   TI
   LI
   LO
   TS
CP0431157
(1-Methanesulfonyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C19H28N2O2S
 1
1
Ki = 52 nM
   TI
   LI
   LO
   TS
CP0216553
N,N-dipropyl-1-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-amine
   Show/Hide
C20H27F3N2
 1
1
Ki = 54 nM
   TI
   LI
   LO
   TS
CP0408685
2-((R)-8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indol-1-yl)-2-oxo-acetamide
   Show/Hide
C20H27N3O2
 1
1
Ki = 54 nM
   TI
   LI
   LO
   TS
CP0501934
4-fluoro-N-(3-{1-[3-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)propyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
   Show/Hide
C43H44F2N6O2
 1
1
Ki = 79 nM
   TI
   LI
   LO
   TS
CP0440286
2-(8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indol-1-yl)-2-oxo-acetamide
   Show/Hide
C20H27N3O2
 1
1
Ki = 87 nM
   TI
   LI
   LO
   TS
CP0430125
1-(8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indol-1-yl)-ethanone
   Show/Hide
C20H28N2O
 1
1
Ki = 108 nM
   TI
   LI
   LO
   TS
CP0497094
1-(8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indol-1-yl)-2,2,2-trifluoro-ethanone
   Show/Hide
C20H25F3N2O
 1
1
Ki = 112 nM
   TI
   LI
   LO
   TS
CP0078427
4-Fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide
   Show/Hide
C21H22FN3O
 1
1
Ki = 137 nM
   TI
   LI
   LO
   TS
CP0425349
4-fluoro-N-{3-[1-({3-[(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)methyl]phenyl}methyl)piperidin-4-yl]-1H-indol-5-yl}benzamide
   Show/Hide
C48H46F2N6O2
 1
1
Ki = 151 nM
   TI
   LI
   LO
   TS
CP0221880
(S)-8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
   Show/Hide
C19H26N2O
 1
1
Ki = 155 nM
   TI
   LI
   LO
   TS
CP0037227
7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
   Show/Hide
C16H25NO
 1
1
Ki = 164 nM
   TI
   LI
   LO
   TS
CP0052478
(+/-)-8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
   Show/Hide
C19H26N2O
 1
1
Ki = 173 nM
   TI
   LI
   LO
   TS
CP0036796
[3-[2-(dipropylamino)ethyl]-1H-indol-5-yl] trifluoromethanesulfonate
   Show/Hide
C17H23F3N2O3S
 1
1
Ki = 190 nM
   TI
   LI
   LO
   TS
CP0495965
(4-Fluoro-3-methyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C19H27FN2
 1
1
Ki = 217 nM
   TI
   LI
   LO
   TS
CP0467900
4-fluoro-N-(3-{1-[2-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)ethyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
   Show/Hide
C42H42F2N6O2
 1
1
Ki = 219 nM
   TI
   LI
   LO
   TS
CP0383969
((S)-4-Fluoro-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl)-dipropyl-amine
   Show/Hide
C18H25FN2
 1
1
Ki = 294 nM
   TI
   LI
   LO
   TS
CP0393209
8-Dipropylamino-3-methyl-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
   Show/Hide
C20H28N2O
 1
1
Ki = 334 nM
   TI
   LI
   LO
   TS
CP0497101
8-Dipropylamino-4-fluoro-3-methyl-6,7,8,9-tetrahydro-3H-benzo[e]indole-1-carbaldehyde
   Show/Hide
C20H27FN2O
 1
1
Ki = 419 nM
   TI
   LI
   LO
   TS
CP0216619
(8S)-N,N-dipropyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-amine
   Show/Hide
C18H26N2
 1
1
Ki = 440 nM
   TI
   LI
   LO
   TS
CP0431098
2-((S)-8-Dipropylamino-6,7,8,9-tetrahydro-3H-benzo[e]indol-1-yl)-2-oxo-acetamide
   Show/Hide
C20H27N3O2
 1
1
Ki = 440 nM
   TI
   LI
   LO
   TS
CP0384025
(6-Fluoro-1,2,3,4-tetrahydro-naphthalen-2-yl)-propyl-amine
   Show/Hide
C13H18FN
 1
1
Ki = 585 nM
   TI
   LI
   LO
   TS
CP0404397
2-Fluoro-N*6*,N*6*-dipropyl-5,6,7,8-tetrahydro-naphthalene-1,6-diamine
   Show/Hide
C16H25FN2
 1
1
Ki = 762 nM
   TI
   LI
   LO
   TS
CP0449397
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-piperazin-1-yl-ethanone
   Show/Hide
C16H22N4O2
 1
1
Ki > 100 nM
   TI
   LI
   LO
   TS
CP0422476
N-[3-[1-[3-amino-2-[4-[5-[(4-fluorobenzoyl)amino]-1H-indol-3-yl]piperidin-1-yl]-3-oxopropyl]piperidin-4-yl]-1H-indol-5-yl]-4-fluorobenzamide
   Show/Hide
C43H43F2N7O3
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0439234
N-[3-(1-benzylpiperidin-4-yl)-1H-indol-5-yl]-4-fluorobenzamide
   Show/Hide
C27H26FN3O
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0439235
4-fluoro-N-(3-(1-octylpiperidin-4-yl)-1H-indol-5-yl)benzamide
   Show/Hide
C28H36FN3O
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0455100
4-fluoro-N-(3-{1-[3,3,3-trifluoro-2-(4-{5-[(4-fluorobenzene)amido]-1H-indol-3-yl}piperidin-1-yl)propyl]piperidin-4-yl}-1H-indol-5-yl)benzamide
   Show/Hide
C43H41F5N6O2
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0457584
10-(4-(5-(4-fluorobenzamido)-1H-indol-3-yl)piperidin-1-yl)decanoic acid
   Show/Hide
C30H38FN3O3
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0467897
N-[3-[1-[3-(dimethylamino)propyl]piperidin-4-yl]-1H-indol-5-yl]-4-fluorobenzamide
   Show/Hide
C25H31FN4O
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0467898
4-fluoro-N-(3-(1-(2-hydroxyethyl)piperidin-4-yl)-1H-indol-5-yl)benzamide
   Show/Hide
C22H24FN3O2
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0497726
4-fluoro-N-(3-(1-(2-(piperidin-1-yl)ethyl)piperidin-4-yl)-1H-indol-5-yl)benzamide
   Show/Hide
C27H33FN4O
 1
1
Ki > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0218850
6-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]-4H-1,4-benzoxazin-3-one
   Show/Hide
C24H26N4O2
 1
1 EC50 = 0.5012 nM
CP0048312
3-(4-{7-[4-(5-carbamoyl-1H-3-indolyl)-3-cyclohexenylamino]heptylamino}-1-cyclohexenyl)-1H-5-indolecarboxamide
   Show/Hide
C37H46N6O2
 1
1 IC50 = 0.05 nM
CP0115159
(S)-4-[3-(2-{(S)-3-[((S)-1-Phenyl-ethylamino)-methyl]-pyrrolidin-1-yl}-ethyl)-1H-indol-5-ylmethyl]-oxazolidin-2-one
   Show/Hide
C27H34N4O2
 1
1 IC50 = 0.3 nM
CP0056703
(S)-4-(3-{2-[(S)-3-(Benzylamino-methyl)-pyrrolidin-1-yl]-ethyl}-1H-indol-5-ylmethyl)-oxazolidin-2-one
   Show/Hide
C26H32N4O2
 1
1 IC50 = 0.35 nM
CP0079840
Benzyl-{(S)-1-[2-(5-[1,2,4]triazol-4-yl-1H-indol-3-yl)-ethyl]-pyrrolidin-3-ylmethyl}-amine
   Show/Hide
C24H28N6
 1
1 IC50 = 0.5 nM
CP0136962
3-(3-{4-[2-(3-Fluoro-phenyl)-ethyl]-piperazin-1-yl}-propyl)-5-[1,2,4]triazol-4-yl-1H-indole
   Show/Hide
C25H29FN6
 1
1 IC50 = 0.6 nM
CP0041353
C-(3-{2-[(S)-3-(Benzylamino-methyl)-pyrrolidin-1-yl]-ethyl}-1H-indol-5-yl)-N-methyl-methanesulfonamide
   Show/Hide
C24H32N4O2S
 1
1 IC50 = 1.1 nM
CP0001238
14C-5-hydroxy tryptamine creatinine disulfate
   Show/Hide
C10H12N2O
 5
1 IC50 = 3 nM
2 Ki = 1.7 nM
3 Ki = 2 nM
4 Ki = 4.8 nM
5 Ki = 5.06 nM
CP0005653
(3-[2-(dimethylamino)ethyl]-1H-indol-5-yl)-N-methylmethanesulfonamide
   Show/Hide
C14H21N3O2S
 10
1 IC50 = 39.81 nM
2 IC50 = 100 nM
3 IC50 = 2400 nM
4 Ki = 3.4 nM
5 Ki = 4.4 nM
6 Ki = 5.5 nM
7 Ki = 8.5 nM
8 Ki = 8.6 nM
9 Ki = 11 nM
10 Ki = 23.1 nM
CP0162751
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-phenyl-piperazin-1-yl)-ethanone
   Show/Hide
C22H26N4O2
 3
1 Ki = 0.4 nM
2 Ki = 0.6 nM
3 Ki = 1.2 nM
CP0056131
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-[4-(3-methoxy-phenyl)-piperazin-1-yl]-ethanone
   Show/Hide
C23H28N4O3
 2
1 Ki = 0.4 nM
2 Ki = 2 nM
CP0106415
2-(5-(2-(8-(4-methylpiperazin-1-yl)naphthalen-2-yloxy)ethoxy)-1H-indol-3-yl)ethanamine
   Show/Hide
C27H32N4O2
 1
1 Ki = 0.4 nM
CP0173138
N-[3-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]phenyl]methanesulfonamide
   Show/Hide
C25H31N3O3S
 1
1 Ki = 0.5012 nM
CP0151604
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-naphthalen-1-yl-piperazin-1-yl)-ethanone
   Show/Hide
C26H28N4O2
 2
1 Ki = 0.52 nM
2 Ki = 0.95 nM
CP0099897
(S)-4-((3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one
   Show/Hide
C16H21N3O2
 3
1 Ki = 0.76 nM
2 Ki = 0.92 nM
3 Ki = 4 nM
CP0079263
2-methyl-5-[2-[4-(quinolin-8-ylmethyl)piperazin-1-yl]ethoxy]quinoline
   Show/Hide
C26H28N4O
 1
1 Ki = 0.7943 nM
CP0102236
2-[3-(2-Amino-ethyl)-1H-indol-5-yloxy]-1-(4-o-tolyl-piperazin-1-yl)-ethanone
   Show/Hide
C23H28N4O2
 4
1 Ki = 0.8 nM
2 Ki = 0.87 nM
3 Ki = 2.08 nM
4 Ki = 2.1 nM
CP0045584
(5'alpha)-12'-hydroxy-2'-methyl-5'-(phenylmethyl)ergotoman-3',6',18-trione
   Show/Hide
C33H35N5O5
 2
1 Ki = 0.8 nM
2 Ki = 6 nM
CP0169227
C-[3-(2-Dimethylamino-ethyl)-1H-indol-5-yl]-N-[4-({[3-(2-dimethylamino-ethyl)-1H-indol-5-ylmethanesulfonyl]-methyl-amino}-methyl)-benzyl]-N-methyl-methanesulfonamide
   Show/Hide
C36H48N6O4S2
 1
1 Ki = 0.89 nM
CP0214664
2-(dimethylamino)-N-[3-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]phenyl]acetamide
   Show/Hide
C28H36N4O2
 1
1 Ki = 1 nM
CP0275909
N-[4-[4-[2-[[3-(2-aminoethyl)-1H-indol-5-yl]oxy]acetyl]piperazin-1-yl]phenyl]acetamide
   Show/Hide
C24H29N5O3
 2
1 Ki = 1.4 nM
2 Ki = 2.8 nM
CP0152118
6-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]-4H-1,4-benzoxazin-3-one
   Show/Hide
C26H29N3O3
 1
1 Ki = 1.585 nM
CP0030068
N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
   Show/Hide
C15H19N5
 3
1 Ki = 4.3 nM
2 Ki = 13.5 nM
3 Ki = 40 nM
CP0061753
1-NP
   Show/Hide
C14H16N2
 1
1 Ki = 6.18 nM
CP0077951
1-(2-(4-(6-fluoro-1H-indol-3-yl)-5,6-dihydropyridin-1(2H)-yl)ethyl)-3,4-dihydro-1H-isochromene-6-carboxamide
   Show/Hide
C25H26FN3O2
 1
1 Ki = 56 nM
CP0037227
7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
   Show/Hide
C16H25NO
 1
1 Ki = 115 nM
CP0078427
4-Fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide
   Show/Hide
C21H22FN3O
 1
1 Ki = 430 nM
CP0096286
(R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidin-1-ylsulfonyl)phenol
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C18H28N2O3S
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( 5-HT 1D receptor (HTR1D) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Migraine [ICD-11: 8A80]
2 Hyperprolactinaemia [ICD-11: 5A60.1]
3 Major depressive disorder [ICD-11: 6A70.3]
Approved Drug(s) 7 Approved Drugs  7
1 Almogran Approved
Migraine
2 Eletriptan Approved
Migraine
3 Frovatriptan Approved
Migraine
4 Metergolin Approved
Hyperprolactinaemia
5 Rizatriptan Approved
Migraine
6 Sumatriptan Approved
Migraine
7 Zolmitriptan Approved
Migraine
Discontinued Drug(s) 7 Discontinued Drugs  7
1 Alniditan Discontinued in Phase 3
Migraine
2 CP-122288 Discontinued in Phase 2
Migraine
3 PNU-142633 Discontinued in Phase 2
Migraine
4 ALX-0646 Discontinued in Phase 1
Migraine
5 GR-127935 Terminated
Major depressive disorder
6 L-694247 Terminated
Migraine
7 PNU-109291 Terminated
Migraine