General Information of the Protein
Protein ID
PT04565
Protein Name
Follicle-stimulating hormone receptor
Secondarily
Protein Name
Follitropin receptor
Gene Name
FSHR
Secondarily
Gene Name
LGR1
Sequence
MALLLVSLLAFLSLGSGCHHRICHCSNRVFLCQESKVTEIPSDLPRNAIELRFVLTKLRVIQKGAFSGFGDLEKIEISQNDVLEVIEADVFSNLPKLHEIRIEKANNLLYINPEAFQNLPNLQYLLISNTGIKHLPDVHKIHSLQKVLLDIQDNINIHTIERNSFVGLSFESVILWLNKNGIQEIHNCAFNGTQLDELNLSDNNNLEELPNDVFHGASGPVILDISRTRIHSLPSYGLENLKKLRARSTYNLKKLPTLEKLVALMEASLTYPSHCCAFANWRRQISELHPICNKSILRQEVDYMTQARGQRSSLAEDNESSYSRGFDMTYTEFDYDLCNEVVDVTCSPKPDAFNPCEDIMGYNILRVLIWFISILAITGNIIVLVILTTSQYKLTVPRFLMCNLAFADLCIGIYLLLIASVDIHTKSQYHNYAIDWQTGAGCDAAGFFTVFASELSVYTLTAITLERWHTITHAMQLDCKVQLRHAASVMVMGWIFAFAAALFPIFGISSYMKVSICLPMDIDSPLSQLYVMSLLVLNVLAFVVICGCYIHIYLTVRNPNIVSSSSDTRIAKRMAMLIFTDFLCMAPISFFAISASLKVPLITVSKAKILLVLFHPINSCANPFLYAIFTKNFRRDFFILLSKCGCYEMQAQIYRTETSSTVHNTHPRNGHCSSAPRVTNGSTYILVPLSHLAQN
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Glycohormone receptor
>
Glycohormone receptor
Function
G protein-coupled receptor for follitropin, the follicle-stimulating hormone (PubMed:11847099, PubMed:24058690, PubMed:24692546). Through cAMP production activates the downstream PI3K-AKT and ERK1/ERK2 signaling pathways (PubMed:24058690).
    Show/Hide
Uniprot ID
Primary ID:
P23945

Secondarily ID:
A0A0A0MSC5
A8K947
G5CBS7
G5E967
J3KQ00
Q05AH0
Q16225
Q4QRJ3
Q4ZFZ2
Q53RW2
    Show/Hide
HGNC ID
HGNC:3969
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
CP0377831
5-amino-N-tert-butyl-2-(methylthio)-4-(3-(2-oxo-2-(prop-2-ynylamino)ethylamino)phenyl)thieno[2,3-d]pyrimidine-6-carboxamide
   Show/Hide
C23H26N6O2S2
 1
1
EC50 = 126 nM
   TI
   LI
   LO
   TS
CP0380316
5-amino-4-(3-(2-((1-(2-(2-(2-azidoethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methylamino)-2-oxoethylamino)phenyl)-N-tert-butyl-2-(methylthio)thieno[2,3-d]pyrimidine-6-carboxamide
   Show/Hide
C29H38N12O4S2
 1
1
EC50 = 397 nM
   TI
   LI
   LO
   TS
CP0391883
1-(6-amino-2,2,4-trimethyl-4-phenyl-3H-quinolin-1-yl)ethanone
   Show/Hide
C20H24N2O
 1
1
EC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0538708
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-4-propylbenzamide
   Show/Hide
C30H34N2O2
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0559356
N-(1-acetyl-2,2,4,7-tetramethyl-4-phenyl-3H-quinolin-6-yl)-4-phenylbenzamide
   Show/Hide
C34H34N2O2
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0500515
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-4-(trifluoromethyl)benzamide
   Show/Hide
C28H27F3N2O2
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0518113
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-3-phenylbenzamide
   Show/Hide
C33H32N2O2
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0435511
Biphenyl-4-carboxylic acid (1-acetyl-2,2,4-trimethyl-4-phenyl-1,2,3,4-tetrahydro-quinolin-6-yl)-amide
   Show/Hide
C33H32N2O2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0378099
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-2-phenylbenzamide
   Show/Hide
C33H32N2O2
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0542108
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)furan-2-carboxamide
   Show/Hide
C25H26N2O3
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0374398
N-(1-acetyl-8-methoxy-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-4-phenylbenzamide
   Show/Hide
C34H34N2O3
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0378864
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-4-chlorobenzamide
   Show/Hide
C27H27ClN2O2
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0380315
(R)-N-(1-acetyl-2,2,4-trimethyl-4-(4-(prop-2-ynyloxy)phenyl)-1,2,3,4-tetrahydroquinolin-6-yl)biphenyl-4-carboxamide
   Show/Hide
C36H34N2O3
 1
1
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0408617
N-[1-acetyl-2,2,4-trimethyl-4-(4-methylphenyl)-3H-quinolin-6-yl]-4-phenylbenzamide
   Show/Hide
C34H34N2O2
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0451717
(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl) 4-phenylbenzoate
   Show/Hide
C33H31NO3
 1
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
CP0538697
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-2-[(2-methylpropan-2-yl)oxy]acetamide
   Show/Hide
C26H34N2O3
 1
1
IC50 = 76 nM
   TI
   LI
   LO
   TS
CP0408618
1-[2,2,4-trimethyl-4-phenyl-6-[(4-phenylphenyl)methoxy]-3H-quinolin-1-yl]ethanone
   Show/Hide
C33H33NO2
 1
1
IC50 = 166 nM
   TI
   LI
   LO
   TS
CP0455572
N-[1-acetyl-4-(2-methoxyphenyl)-2,2,4-trimethyl-3H-quinolin-6-yl]-4-phenylbenzamide
   Show/Hide
C34H34N2O3
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0559355
N-[1-acetyl-4-(4-hydroxyphenyl)-2,2,4-trimethyl-3H-quinolin-6-yl]-4-phenylbenzamide
   Show/Hide
C33H32N2O3
 1
1
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0393745
(R)-N-(1-acetyl-4-(4-((1-(2-(2-(2-azidoethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-2,2,4-trimethyl-1,2,3,4-tetrahydroquinolin-6-yl)biphenyl-4-carboxamide
   Show/Hide
C42H46N8O5
 1
1
IC50 = 324 nM
   TI
   LI
   LO
   TS
CP0554570
1-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-3-phenylurea
   Show/Hide
C27H29N3O2
 1
1
IC50 = 580 nM
   TI
   LI
   LO
   TS
CP0377834
(R)-4-(3-(2-((1-(2-(2-(2-(4-((4-(1-acetyl-6-biphenyl-4-ylcarboxamido-2,2,4-trimethyl-1,2,3,4-tetrahydroquinolin-4-yl)phenoxy)methyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methylamino)-2-oxoethylamino)phenyl)-5-amino-N-tert-butyl-2-(methylthio)thieno[2,3-d]pyrimidine-6-carboxamide
   Show/Hide
C65H72N14O7S2
 1
1
IC50 = 920 nM
   TI
   LI
   LO
   TS
CP0511876
1-[6-[(4-tert-butylphenyl)methylamino]-2,2,4-trimethyl-4-phenyl-3H-quinolin-1-yl]ethanone
   Show/Hide
C31H38N2O
 1
1
IC50 = 930 nM
   TI
   LI
   LO
   TS
CP0393737
(R)-4-(3-(2-((1-(14-(4-((4-(1-acetyl-6-biphenyl-4-ylcarboxamido-2,2,4-trimethyl-1,2,3,4-tetrahydroquinolin-4-yl)phenoxy)methyl)-1H-1,2,3-triazol-1-yl)-3,6,9,12-tetraoxatetradecyl)-1H-1,2,3-triazol-4-yl)methylamino)-2-oxoethylamino)phenyl)-5-amino-N-tert-butyl-2-(methylthio)thieno[2,3-d]pyrimidine-6-carboxamide
   Show/Hide
C69H80N14O9S2
 1
1
IC50 = 1023 nM
   TI
   LI
   LO
   TS
CP0377830
(R)-4-(3-(2-((1-(2-(2-(2-(2-(4-((4-(1-acetyl-6-biphenyl-4-ylcarboxamido-2,2,4-trimethyl-1,2,3,4-tetrahydroquinolin-4-yl)phenoxy)methyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methylamino)-2-oxoethylamino)phenyl)-5-amino-N-tert-butyl-2-(methylthio)thieno[2,3-d]pyrimidine-6-carboxamide
   Show/Hide
C67H76N14O8S2
 1
1
IC50 = 1662 nM
   TI
   LI
   LO
   TS
CP0554571
1-acetyl-N-[2-(4-methoxyphenyl)ethyl]-2,2,4-trimethyl-4-phenyl-3H-quinoline-6-carboxamide
   Show/Hide
C30H34N2O3
 1
1
IC50 = 1880 nM
   TI
   LI
   LO
   TS
CP0378100
N-(1-acetyl-2,2,4-trimethyl-4-phenyl-3H-quinolin-6-yl)-1-phenylmethanesulfonamide
   Show/Hide
C27H30N2O3S
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Follicle-stimulating hormone receptor (FSHR) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 African trypanosomiasis [ICD-11: 1F51]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Suramin Phase 1
African trypanosomiasis