Ki Summary

Reaction Details

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Target

Corticotropin-releasing factor receptor 1

Ligand

BDBM50131716

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_51128 (CHEMBL663563)

1.9±n/a nM

Citation

Jagoda, E; Contoreggi, C; Lee, MJ; Kao, CH; Szajek, LP; Listwak, S; Gold, P; Chrousos, G; Greiner, E; Kim, BM; Jacobson, AE; Rice, KC; Eckelman, W Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2. J Med Chem46:3559-62 (2003) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Corticotropin-releasing factor receptor 1

Name:

Corticotropin-releasing factor receptor 1

Synonyms:

Type:

G Protein-Coupled Receptor (GPCR)

Mol. Mass.:

47870.75

Organism:

Rattus norvegicus (rat)

Description:

Receptor binding assays were performed using rat cortex homogenate.

Residue:

415

Sequence:

MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEV
HQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPF
PIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRA
STTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVS
VFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV

BDBM50131716

n/a

Name

BDBM50131716

Synonyms:

CHEMBL430892 | [3-(4-Bromo-2-chloro-phenyl)-2,5-dimethyl-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-yl]-bis-(2-methoxy-ethyl)-amine

Type

Small organic molecule

Emp. Form.

C19H23BrClN5O2

Mol. Mass.

468.775

SMILES

COCCN(CCOC)c1nc(C)nc2c(c(C)nn12)-c1ccc(Br)cc1Cl |(2.5,2.36,;1.17,3.13,;-.17,2.36,;-1.5,3.12,;-2.85,2.35,;-4.18,3.11,;-5.51,2.34,;-6.84,3.11,;-8.17,2.34,;-2.83,.81,;-4.16,.04,;-4.16,-1.51,;-5.51,-2.28,;-2.83,-2.28,;-1.49,-1.5,;-.03,-1.98,;.88,-.73,;2.42,-.73,;-.03,.52,;-1.49,.04,;.44,-3.44,;-.59,-4.58,;-.12,-6.04,;1.39,-6.36,;1.87,-7.83,;2.43,-5.21,;1.94,-3.75,;2.96,-2.61,)|

Structure