General Information of the Protein
Protein ID
PT02242
Protein Name
Gastric inhibitory polypeptide receptor
Secondarily
Protein Name
Glucose-dependent insulinotropic polypeptide receptor
Gene Name
GIPR
Sequence
MTTSPILQLLLRLSLCGLLLQRAETGSKGQTAGELYQRWERYRRECQETLAAAEPPSGLACNGSFDMYVCWDYAAPNATARASCPWYLPWHHHVAAGFVLRQCGSDGQWGLWRDHTQCENPEKNEAFLDQRLILERLQVMYTVGYSLSLATLLLALLILSLFRRLHCTRNYIHINLFTSFMLRAAAILSRDRLLPRPGPYLGDQALALWNQALAACRTAQIVTQYCVGANYTWLLVEGVYLHSLLVLVGGSEEGHFRYYLLLGWGAPALFVIPWVIVRYLYENTQCWERNEVKAIWWIIRTPILMTILINFLIFIRILGILLSKLRTRQMRCRDYRLRLARSTLTLVPLLGVHEVVFAPVTEEQARGALRFAKLGFEIFLSSFQGFLVSVLYCFINKEVQSEIRRGWHHCRLRRSLGEEQRQLPERAFRALPSGSGPGEVPTSRGLSSGTLPGPGNEASRELESYC
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family B G protein-coupled receptor
>
Peptide receptor (family B GPCR)
>
Glucagon-like receptor
>
Gastric inhibitory polypeptide receptor
Function
This is a receptor for GIP. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
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Uniprot ID
Primary ID:
P48546

Secondarily ID:
B7WP14
B7ZKQ0
Q14401
Q16400
Q52M04
Q9UPI1
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Ensembl ID
ENSG00000010310
HGNC ID
HGNC:4271
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: CL000051 , BHK-21
Compound ID Compound Name Compound Formula
CP0463788
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(4-trifluoromethylsulfanylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H32F3N3O5S
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0435017
3-(4-((1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
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C29H36F3N3O5
 1
1
IC50 = 28.3 nM
   TI
   LI
   LO
   TS
CP0500823
3-{4-[1-(4-tert-Butylphenyl)-3-(4-trifluoromethoxyphenyl)ureidomethyl]benzoylamino}propionicacid
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C29H30F3N3O5
 1
1
IC50 = 38 nM
   TI
   LI
   LO
   TS
CP0211346
3-(4-((1-(4-cyclohexenylphenyl)-3-(3,5-dichlorophenyl)ureido)methyl)benzamido)propanoic acid
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C30H29Cl2N3O4
 1
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
CP0459787
(R)-3-{4-[3-(3-tert-Butylphenyl)-1-(4-cyclohexylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C34H41N3O5
 1
1
IC50 = 74 nM
   TI
   LI
   LO
   TS
CP0503148
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(2,2,4,4-tetrafluoro-4H-benzo[1,3]dioxin-6-yl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C32H29F4N3O7
 1
1
IC50 = 83 nM
   TI
   LI
   LO
   TS
CP0383869
(R)-trans-3-{4-[3-(3,5-Bis(trifluoromethyl)phenyl)-1-(4-tert-butylcyclohexyl)ureidomethyl]-benzoylamino}-2-hydroxypropionic acid
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C30H35F6N3O5
 1
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0430821
3-[[4-[[[3,5-bis(trifluoromethyl)phenyl]carbamoyl-(4-tert-butylcyclohexyl)amino]methyl]benzoyl]amino]propanoic acid
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C30H35F6N3O4
 1
1
IC50 = 93 nM
   TI
   LI
   LO
   TS
CP0441152
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H31Cl2N3O5
 1
1
IC50 = 93 nM
   TI
   LI
   LO
   TS
CP0423784
(R)-trans-3-{4-[1-(4-tert-Butyl-cyclohexyl)-3-(3-methyl-5-trifluoromethylphenyl)ureidomethyl]benzoylamino}-2-hydroxy-propionic acid
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C30H38F3N3O5
 1
1
IC50 = 98 nM
   TI
   LI
   LO
   TS
CP0497971
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(3-methoxy-5-trifluoromethylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionicacid
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C32H34F3N3O6
 1
1
IC50 = 145 nM
   TI
   LI
   LO
   TS
CP0517419
(R)-3-{4-[3-(4-Cyano-3-trifluoromethylphenyl)-1-(4-cyclohexylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C32H31F3N4O5
 1
1
IC50 = 198 nM
   TI
   LI
   LO
   TS
CP0443414
aminothiazole, 3
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C33H30F3N3O4S
 1
1
IC50 = 207 nM
   TI
   LI
   LO
   TS
CP0374456
thiazole, 27
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C28H22ClF3N2O3S
 2
1
IC50 = 211 nM
   TI
   LI
   LO
   TS
2
IC50 = 381 nM
   TI
   LI
   LO
   TS
CP0459789
(R)-3-{4-[3-(3-Bromophenyl)-1-(4-cyclohexylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H32BrN3O5
 1
1
IC50 = 216 nM
   TI
   LI
   LO
   TS
CP0387508
(R)-trans-3-{4-[1-(4-tert-Butylcyclohexyl)-3-(3,5-dimethylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H41N3O5
 1
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0375059
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3-fluoro-5-trifluoromethylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H29F4N3O5
 1
1
IC50 = 277 nM
   TI
   LI
   LO
   TS
CP0454980
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3-methoxy-5-trifluoromethylphenyl)ureidomethyl]-benzoylamino}-2-hydroxypropionic acid
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C32H32F3N3O6
 1
1
IC50 = 279 nM
   TI
   LI
   LO
   TS
CP0443411
aminothiazole, 6
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C34H26F3N3O4S
 2
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
2
IC50 = 488 nM
   TI
   LI
   LO
   TS
CP0443412
aminothiazole, 12
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C31H30F3N3O3S
 2
1
IC50 = 293 nM
   TI
   LI
   LO
   TS
2
IC50 = 633 nM
   TI
   LI
   LO
   TS
CP0462530
(R/S)-3-{4-[1-(4-tert-Butylphenyl)-3-(4-trifluoromethoxyphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C29H30F3N3O6
 1
1
IC50 = 315 nM
   TI
   LI
   LO
   TS
CP0494614
thiazole, 29
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C28H22ClF3N2O4S
 1
1
IC50 = 316 nM
   TI
   LI
   LO
   TS
CP0374455
aminothiazole, 24
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C33H26ClN3O3S
 2
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
2
IC50 = 555 nM
   TI
   LI
   LO
   TS
CP0070503
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H29Cl2N3O5
 1
1
IC50 = 359 nM
   TI
   LI
   LO
   TS
CP0475018
aminothiazole, 4
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C33H30F3N3O3S
 1
1
IC50 = 368 nM
   TI
   LI
   LO
   TS
CP0497970
(S)-trans-3-{4-[3-(3,5-Bis(trifluoromethyl)phenyl)-1-(4-tert-butylcyclohexyl)ureidomethyl]-benzoylamino}-2-hydroxypropionic acid
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C30H35F6N3O5
 1
1
IC50 = 373 nM
   TI
   LI
   LO
   TS
CP0459788
(R)-3-{4-[3-(3-Bromo-5-trifluoromethylphenyl)-1-(4-cyclohex-1-enylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H29BrF3N3O5
 1
1
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0435234
aminothiazole, 1
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C32H31N3O3S
 1
1
IC50 = 389 nM
   TI
   LI
   LO
   TS
CP0374482
aminothiazole, 10
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C30H27Cl2N3O3S
 2
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
2
IC50 = 830 nM
   TI
   LI
   LO
   TS
CP0443415
aminothiazole, 11
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C31H28F3N3O3S
 2
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
2
IC50 = 564 nM
   TI
   LI
   LO
   TS
CP0375060
(R)-3-{4-[3-(3-Chlorophenyl)-1-(4-cyclohex-1-enylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H30ClN3O5
 1
1
IC50 = 406 nM
   TI
   LI
   LO
   TS
CP0475021
aminothiazole, 16
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C27H21ClF3N3O3S
 2
1
IC50 = 410 nM
   TI
   LI
   LO
   TS
2
IC50 = 649 nM
   TI
   LI
   LO
   TS
CP0435018
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(3-methylthio)phenyl-ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H35N3O5S
 1
1
IC50 = 411 nM
   TI
   LI
   LO
   TS
CP0475022
thiazole, 28
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C28H22ClF3N2O4S
 1
1
IC50 = 429 nM
   TI
   LI
   LO
   TS
CP0466540
(S)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H29Cl2N3O5
 1
1
IC50 = 445 nM
   TI
   LI
   LO
   TS
CP0443416
aminothiazole, 17
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C27H21ClF3N3O4S
 2
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
2
IC50 = 869 nM
   TI
   LI
   LO
   TS
CP0468561
aminothiazole, 19
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C28H21F6N3O4S
 2
1
IC50 = 480 nM
   TI
   LI
   LO
   TS
2
IC50 = 833 nM
   TI
   LI
   LO
   TS
CP0462586
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3-methanesulfonyl-4-trifluoromethoxyphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C32H32F3N3O8S
 1
1
IC50 = 497 nM
   TI
   LI
   LO
   TS
CP0494615
aminothiazole, 7
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C30H26F3N3O3S
 2
1
IC50 = 510 nM
   TI
   LI
   LO
   TS
2
IC50 = 1095 nM
   TI
   LI
   LO
   TS
CP0495973
thiazole, 30
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C29H22F6N2O5S
 1
1
IC50 = 565 nM
   TI
   LI
   LO
   TS
CP0374471
aminothiazole, 13
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C32H29F6N3O3S
 1
1
IC50 = 584 nM
   TI
   LI
   LO
   TS
CP0485224
aminothiazole, 9
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C29H25Cl2N3O3S
 1
1
IC50 = 638 nM
   TI
   LI
   LO
   TS
CP0495975
aminothiazole, 25
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C34H26F3N3O3S
 1
1
IC50 = 645 nM
   TI
   LI
   LO
   TS
CP0423783
(R/S)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H29Cl2N3O5
 1
1
IC50 = 701 nM
   TI
   LI
   LO
   TS
CP0485223
aminothiazole, 2
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C36H39N3O3S
 1
1
IC50 = 721 nM
   TI
   LI
   LO
   TS
CP0547270
aminothiazole, 14
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C34H39N3O3S
 1
1
IC50 = 729 nM
   TI
   LI
   LO
   TS
CP0445398
aminothiazole, 26
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C34H26F3N3O4S
 1
1
IC50 = 732 nM
   TI
   LI
   LO
   TS
CP0443417
aminothiazole, 8
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C30H26F3N3O4S
 2
1
IC50 = 770 nM
   TI
   LI
   LO
   TS
2
IC50 = 950 nM
   TI
   LI
   LO
   TS
CP0374454
aminothiazole, 21
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C28H21F6N3O3S2
 1
1
IC50 = 777 nM
   TI
   LI
   LO
   TS
CP0468560
aminothiazole, 18
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C27H21ClF3N3O3S
 2
1
IC50 = 990 nM
   TI
   LI
   LO
   TS
2
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0374468
aminothiazole, 5
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C38H34ClN3O3S
 1
1
IC50 = 1002 nM
   TI
   LI
   LO
   TS
CP0445452
aminothiazole, 15
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C30H27Cl2N3O3S
 1
1
IC50 = 1113 nM
   TI
   LI
   LO
   TS
CP0375061
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-phenyl-ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H31N3O5
 1
1
IC50 = 1392 nM
   TI
   LI
   LO
   TS
CP0423785
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-methoxypropionic acid
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C31H31Cl2N3O5
 1
1
IC50 = 3020 nM
   TI
   LI
   LO
   TS
CP0443413
aminothiazole, 20
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C28H24F3N3O4S2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0485225
aminothiazole, 23
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C30H26F3N3O4S
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0495972
aminothiazole, 22
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C30H26F3N3O5S
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Gastric inhibitory polypeptide receptor (GIPR) )
Target Type Successful Target