General Information of the Protein
Protein ID
PT01670
Protein Name
Calcitonin gene-related peptide type 1 receptor
Secondarily
Protein Name
Calcitonin receptor-like receptor
Gene Name
CALCRL
Secondarily
Gene Name
CGRPR
Sequence
MEKKCTLYFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQAEGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRTWTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNLFFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTLIVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICAALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKIAEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSASYTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family B G protein-coupled receptor
>
Peptide receptor (family B GPCR)
>
Calcitonin-like receptor
>
Calcitonin gene-related peptide receptor
Function
Receptor for calcitonin-gene-related peptide (CGRP) together with RAMP1 and receptor for adrenomedullin together with RAMP3 (By similarity). Receptor for adrenomedullin together with RAMP2 (PubMed:22102369, PubMed:30115739). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase (PubMed:22102369, PubMed:30115739).
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Uniprot ID
Primary ID:
Q16602

Secondarily ID:
A8K6G5
A8KAD3
Q53S02
Q53TS5
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Ensembl ID
ENSG00000064989
HGNC ID
HGNC:16709
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
CP0920825
 Compound Info 
(S)-1-((3S,6S,9S,12S,18S,24S)-1-((S)-1-((5S,8S,14S,17S,20S,23S,26S,29S,32S,35S,38S,41S,44S,47S)-41-((1H-imidazol-5-yl)methyl)-5-((4R,7S,10S,13S,16S,22R)-22-amino-16-(2-amino-2-oxoethyl)-7-((R)-1-hydroxyethyl)-10-(hydroxymethyl)-13-isobutyl-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexaazacyclotricosane-4-carboxamido)-32-(2-amino-2-oxoethyl)-23-(3-amino-3-oxopropyl)-35-(4-aminobutyl)-29,38,47-tribenzyl-26-(carboxymethyl)-17-(4-hydroxybenzyl)-14,20-bis((R)-1-hydroxyethyl)-44-((S)-1-hydroxyethyl)-8-isobutyl-6,9,12,15,18,21,24,27,30,33,36,39,42,45-tetradecaoxo-2-thia-7,10,13,16,19,22,25,28,31,34,37,40,43,46-tetradecaazaoctatetracontane)pyrrolidin-2-yl)-3-(3-amino-3-oxopropyl)-12-sec-butyl-6-((R)-1-hydroxyethyl)-18-isopropyl-9,24-dimethyl-1,4,7,10,13,16,19,22-octaoxo-2,5,8,11,14,17,20,23-octaazapentacosane)pyrrolidine-2-carboxylic acid
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C151H225N39O46S3
  1
1
IC50 = 0.032 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000748 , NAL1A clone C4E10
 Cell Line Info 
Cell Line ID: CL000074 , SK-N-MC
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0000982
 Compound Info 
N-[(2R)-1-[[(2S)-6-amino-1-oxo-1-(4-pyridin-4-ylpiperazin-1-yl)hexan-2-yl]amino]-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxopropan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide
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C38H47Br2N9O5
  5
1 IC50 = 0.03 nM
2 Kd = 0.03981 nM
3 Kd = 0.07943 nM
4 Ki = 0.01 nM
5 Ki = 0.014 nM
CP0024947
 Compound Info 
N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide
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C26H27F5N6O3
  4
1 Kd = 1.9 nM
2 Kd = 3.715 nM
3 Ki = 0.77 nM
4 Ki = 0.8 nM
CP0184709
 Compound Info 
(R)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide
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C35H45FN8O3
  1
1 Ki = 0.013 nM
CP0003456
 Compound Info 
2-[(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide
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C31H29F2N5O3
  1
1 Ki = 0.021 nM
CP0697885
 Compound Info 
(S)-4-chloro-7-(2-oxo-2-(4-(2-oxo-4,5-dihydro-1H-benzo[d][1,3]diazepin-3(2H)-yl)piperidin-1-yl)ethyl)-9-(2,2,2-trifluoroethyl)-6,7,9,10-tetrahydroazepino[3,4-e]indazol-8(3H)-one
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C29H30ClF3N6O3
  1
1 Ki = 0.1 nM
CP0184708
 Compound Info 
(R)-N-(1-(1,4'-bipiperidin-1'-yl)-3-(1H-indazol-5-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamide
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C34H44N8O3
  1
1 Ki = 0.23 nM
CP0327608
 Compound Info 
(S)-N-benzyl-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H30N4O4
  1
1 Ki = 1.9 nM
CP0134898
 Compound Info 
(R)-4-(2-oxo-2,3-dihydroimidazo[4,5-b]pyridin-1-yl)-N-(2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)piperidine-1-carboxamide
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C29H26F3N7O3
  1
1 Ki = 23 nM
CP0668570
 Compound Info 
(R)-4-(2,4-dioxoimidazolidin-1-yl)-N-(2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)piperidine-1-carboxamide
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C26H25F3N6O4
  1
1 Ki = 29 nM
CP0013441
 Compound Info 
(R)-4-(2-oxo-2,3-dihydrobenzo[d]imidazol-1-yl)-N-(2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)piperidine-1-carboxamide
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C30H27F3N6O3
  1
1 Ki = 2250 nM
Clinical Information about the Protein
Target 1 ( Calcitonin gene-related peptide receptor (CGRPR) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Migraine [ICD-11: 8A80]
2 Cluster headache [ICD-11: 8A81.0]
Approved Drug(s) 4 Approved Drugs  4
1 Rimegepant
 Drug Info 
Approved
Migraine
2 Ubrogepant
 Drug Info 
Approved
Migraine
3 Atogepant
 Drug Info 
Approved
Migraine
4 Zavegepant
 Drug Info 
Approved
Migraine
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 MK-3207
 Drug Info 
Phase 2
Migraine
2 Olcegepant
 Drug Info 
Phase 2
Migraine
3 Telcagepant
 Drug Info 
Phase 2
Cluster headache
Investigative Drug(s) 1 Investigative Drug  1
1 BMS-694153
 Drug Info 
Investigative
Migraine
Target 2 ( HUMAN calcitonin gene-related peptide type 1 receptor (CALCRL) )
Target Type Unknown Type Target