Details of the Target

General Information of Target

Target ID LDTP03630
Target Name Gastrin/cholecystokinin type B receptor (CCKBR)
Gene Name CCKBR
Gene ID 887
Synonyms
CCKRB; Gastrin/cholecystokinin type B receptor; CCK-B receptor; CCK-BR; Cholecystokinin-2 receptor; CCK2-R
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
PDEDPPTPSIASLSRLSYTTISTLGPG
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
Receptor for gastrin and cholecystokinin. The CCK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.; Isoform 2 is constitutively activated and may regulate cancer cell proliferation via a gastrin-independent mechanism.
TTD ID
T05849
Uniprot ID
P32239
DrugMap ID
TTVFO0U
Ensemble ID
ENST00000334619.7
HGNC ID
HGNC:1571
ChEMBL ID
CHEMBL298

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CALU6 SNV: p.D422Y .
CORL23 SNV: p.R356H .
ICC10 Deletion: p.L249RfsTer3 .
ICC106 Deletion: p.L249RfsTer3 .
ICC108 Deletion: p.L249RfsTer3 .
Ishikawa (Heraklio) 02 ER Deletion: p.L344CfsTer35
SNV: p.P281A		 .
JHH4 SNV: p.R213W .
KP4 SNV: p.V233I .
MDAMB157 SNV: p.V339L .
MEWO SNV: p.A235V .
NCIH1155 SNV: p.A62V .
NCIH446 SNV: p.P361A .
OVISE SNV: p.R213W .
PANC1 SNV: p.A171V .
RKO SNV: p.R158Ter .
SW480 SNV: p.L247I .
UACC257 SNV: p.V286I .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		N.A.  LDD0162  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tyrosine-protein phosphatase non-receptor type 11 (PTPN11) Protein-tyrosine phosphatase family Q06124
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Neurotrimin (NTM) IgLON family Q9P121

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ceruletide Small molecular drug D0Y9TS
Pentagastrin Small molecular drug D0O5TQ
Cholecystokinin . DB08862
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gastrazole Small molecular drug D09XUH
Phase 2
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dexloxiglumide Small molecular drug D0TL7L
Itriglumide Small molecular drug D0K2RY
Spiroglumide Small molecular drug D04KHY
Yf-476 Small molecular drug D0H7FW
Z 360 Small molecular drug D02RPK
S-0509 . D0H5WM
Tt-223 . D02FYE
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Demogastrin . D0QJ6L
Preclinical
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jnj-26070109 Small molecular drug D0E8QK
Pd-170292 Small molecular drug D06DPS
Gg-8573 . D0W4OZ
Investigative
Click To Hide/Show 58 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Small molecular drug D0T2RY
Bc-264 Small molecular drug D0Z4HK
Cck-33 Small molecular drug D05OUQ
Cck-8 Small molecular drug D0I8AF
Ci-1015 Small molecular drug D0C2KS
Desulfated Cholecystokinin-8 Small molecular drug D02VGS
Gw-5823 Small molecular drug D02ZML
Pbc-264 Small molecular drug D0L9RP
Pd-135118 Small molecular drug D0O0IZ
Pd-135158 Small molecular drug D0D2ZM
Pd-136621 Small molecular drug D04VOM
Pd-137337 Small molecular drug D0E4JX
Pd-137342 Small molecular drug D0G7RE
Pd-138915 Small molecular drug D02MIN
Pd-138916 Small molecular drug D0L9OU
Pd-138917 Small molecular drug D0A9EA
Pd-140547 Small molecular drug D00FLQ
Pd-140548 Small molecular drug D08EYZ
Pd-140723 Small molecular drug D0G1CK
Pd-149164 Small molecular drug D08VRJ
Rb-400 Small molecular drug D09TNC
Rp-69758 Small molecular drug D0U5NA
Rp73870 Small molecular drug D0Y8KY
Tetragastrin Small molecular drug D05XXE
Tetronothiodin Small molecular drug D0R4TA
Tp-680 Small molecular drug D0ES2U
Tyr-d-ala-gly-d-trp-nle-asp-phe-nh2 Small molecular drug D06BRA
Tyr-d-ala-gly-d-trp-nmenle-asp-phe-nh2 Small molecular drug D07ICW
Tyr-d-ala-gly-trp-nle-asp-phe-nh2 Small molecular drug D0U6OA
Tyr-d-ala-gly-trp-nmenle-asp-phe-nh2 Small molecular drug D0R4GI
Tyr-d-nle-gly-d-trp-nle-asp-phe-nh2 Small molecular drug D0V0RB
Tyr-d-nle-gly-d-trp-nmenle-asp-phe-nh2 Small molecular drug D0E2OG
Tyr-d-nle-gly-trp-nle-asp-phe-nh2 Small molecular drug D07LQQ
Tyr-d-nle-gly-trp-nmenle-asp-phe-nh2 Small molecular drug D08QKT
Tyr-d-phe-gly-d-trp-nle-asp-phe-nh2 Small molecular drug D09EMR
Tyr-d-phe-gly-d-trp-nmenle-asp-phe-nh2 Small molecular drug D0TR0U
Tyr-d-phe-gly-trp-nle-asp-phe-nh2 Small molecular drug D03EPA
Tyr-d-phe-gly-trp-nmenle-asp-phe-nh2 Small molecular drug D01AQC
Tyr-d-pro-gly-trp-nmenle-asp-phe-nh2 Small molecular drug D01ADK
Tyr-gly-gly-trp-nmenle-asp-phe-nh2 Small molecular drug D0X7LC
Tyr-pro-gly-trp-nmenle-asp-phe-nh2 Small molecular drug D06NIP
[125i]-bdz2 Small molecular drug D0Z4SS
[125i]Pd142308 Small molecular drug D02ZWC
[3h]Jb-93182 Small molecular drug D0F5WV
[3h]Pbc-264 Small molecular drug D0J0NS
[3h]Pd140376 Small molecular drug D0IU6I
Asp-tyr(Oso3h)-met-gly-trp-met-asp-phe . D0CE9U
Boc-asp-tyr(So3-)-nle-gly-trp-asp-phe-nh2 . D0M6ZF
Cholecystokinin-9 . D0A7RT
H-tyr-d-ala-gly-phe-nh-nh-d-trp-nle-asp-phe-bo . D0S7SO
H-tyr-d-ala-gly-phe-nh-nh-d-trp-nle-asp-phe-h . D0V9DY
H-tyr-d-ala-gly-phe-nh-nh-phe-asp-nle-d-trp-h . D0J7GJ
H-tyr-d-ala-gly-phe-nh-nh-phe-asp-nle-trp-ac . D03WGS
H-tyr-d-ala-gly-phe-nh-nh-phe-asp-nle-trp-boc . D0N6DN
Rp-71483 . D0O0AR
Rp-72540 . D06WOQ
Rpr-107836 . D00UPU
Tyr-d-ala-gly-phe-nh-nh-phe-asp-nmenle-d-trp-boc . D0QP2S
Discontinued
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ag-041r Small molecular drug D07SXO
Cr-2093 Small molecular drug D07YHY
Fr-208419 Small molecular drug D01ZDR
Gr-199114x Small molecular drug D0EG1F
Gv-150013 Small molecular drug D0X4AV
Iqm-95333 Small molecular drug D05HGU
L-365260 Small molecular drug D0Z1RQ
Ly288513 Small molecular drug D00UEG
Pd-134308 Small molecular drug D0XJ0S
Pd-135666 Small molecular drug D0I3BT
Pd136450 Small molecular drug D00COB
Ym-022 Small molecular drug D05HYL
Snf-9007 . D0W8TS

References

1 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060