Ki Summary

Reaction Details

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Target

Corticotropin-releasing factor receptor 1

Ligand

BDBM50084875

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_572700 (CHEMBL1026899)

IC50

1.2±n/a nM

Citation

Hartz, RA; Ahuja, VT; Rafalski, M; Schmitz, WD; Brenner, AB; Denhart, DJ; Ditta, JL; Deskus, JA; Yue, EW; Arvanitis, AG; Lelas, S; Li, YW; Molski, TF; Wong, H; Grace, JE; Lentz, KA; Li, J; Lodge, NJ; Zaczek, R; Combs, AP; Olson, RE; Mattson, RJ; Bronson, JJ; Macor, JE In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. J Med Chem52:4161-72 (2009) [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

BDBM50084875

n/a

Name

BDBM50084875

Synonyms:

8-(2,4-dichlorophenyl)-N-(1,3-dimethoxypropan-2-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine | CHEMBL44698 | DMP-696 | DMP696 | [8-(2,4-dichloro-phenyl)-2,7-dimethyl-pyrazolo[1,5-a][1,3,5]triazin-4-yl]-(2-methoxy-1-methoxymethyl-ethyl)-amine

Type

Small organic molecule

Emp. Form.

C18H21Cl2N5O2

Mol. Mass.

410.298

SMILES

COCC(COC)Nc1nc(C)nc2c(c(C)nn12)-c1ccc(Cl)cc1Cl |(-3.04,-6.69,;-3.03,-8.23,;-4.37,-9,;-4.37,-10.54,;-3.03,-11.31,;-1.7,-10.54,;-1.7,-9.01,;-5.7,-11.31,;-5.7,-12.85,;-7.03,-13.63,;-7.03,-15.17,;-8.36,-15.94,;-5.7,-15.93,;-4.37,-15.17,;-2.91,-15.64,;-2,-14.4,;-.46,-14.4,;-2.91,-13.15,;-4.37,-13.63,;-2.18,-17.01,;-3.01,-18.3,;-2.29,-19.67,;-.75,-19.73,;-.03,-21.08,;.06,-18.41,;-.65,-17.05,;.16,-15.75,)|

Structure