Reaction Details |
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Target | Cholecystokinin receptor type A/Gastrin/cholecystokinin type B receptor |
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Ligand | BDBM50227024 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_49422 (CHEMBL658782) |
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IC50 | 100000±n/a nM |
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Citation | Bock, MG; DiPardo, RM; Evans, BE; Rittle, KE; Freidinger, RM; Chang, RS; Lotti, VJ Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted 1,4-benzodiazepin-2-amines. J Med Chem31:264-8 (1988) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Cholecystokinin receptor type A/Gastrin/cholecystokinin type B receptor |
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Name: | Cholecystokinin receptor type A/Gastrin/cholecystokinin type B receptor |
Synonyms: | Cholecystokinin receptor |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 357790 |
Components: | This complex has 2 components. |
Component 1 |
Name: | Cholecystokinin receptor type A |
Synonyms: | CCK-A receptor | CCK-AR | CCK1-R | CCKAR | CCKAR_HUMAN | CCKRA | Cholecystokinin receptor | Cholecystokinin receptor type A | Cholecystokinin-1 Receptor |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 47859.34 |
Organism: | Homo sapiens (Human) |
Description: | Stable expression of human CCK-1 receptors in HEK 293 cells. |
Residue: | 428 |
Sequence: | MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNT
LVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYF
MGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYS
NLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGI
KFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNS
SAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSY
TSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSH
MSASVPPQ
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Component 2 |
Name: | Gastrin/cholecystokinin type B receptor |
Synonyms: | CCK-2 receptor | CCK-B receptor | CCK-BR | CCKBR | CCKRB | Cholecystokinin A | Cholecystokinin receptor | Cholecystokinin-2 Receptor | GASR_HUMAN | Gastrin/cholecystokinin type B receptor |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 48445.79 |
Organism: | Homo sapiens (Human) |
Description: | Stable expression of human CCK-2 receptors in HEK 293 cells. |
Residue: | 447 |
Sequence: | MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
PDEDPPTPSIASLSRLSYTTISTLGPG
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BDBM50227024 |
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n/a |
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Name | BDBM50227024 |
Synonyms: | CHEMBL316238 |
Type | Small organic molecule |
Emp. Form. | C27H25FN4 |
Mol. Mass. | 424.5126 |
SMILES | CCCNC1=Nc2ccccc2C(=N[C@@H]1Cc1c[nH]c2ccccc12)c1ccccc1F |c:13,t:4| |
Structure |
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