Ki Summary

Reaction Details

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Target

Bile acid receptor

Ligand

BDBM30329

Substrate/Competitor

Biotinylated SRC-1 Peptide

Meas. Tech.

FXR Ligand-Seeking Assay

7.5±n/a

Temperature

295.15±n/a K

EC50

87±n/a nM

Comments

134% efficacy.

Citation

Akwabi-Ameyaw, A; Bass, JY; Caldwell, RD; Caravella, JA; Chen, L; Creech, KL; Deaton, DN; Jones, SA; Kaldor, I; Liu, Y; Madauss, KP; Marr, HB; McFadyen, RB; Miller, AB; Iii, FN; Parks, DJ; Spearing, PK; Todd, D; Williams, SP; Wisely, GB Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett18:4339-43 (2008) [PubMed] Article

More Info.:

Get all data from this article, Inhibition_Run data, Solution Info, Assay Method

Bile acid receptor

Name:

Bile acid receptor

Synonyms:

BAR | Bile acid receptor FXR | FXR | Farnesol receptor HRR-1 | HRR1 | NR1H4 | NR1H4_HUMAN | Nuclear receptor subfamily 1 group H member 4 | RIP14 | RXR-interacting protein 14 | Retinoid X receptor-interacting protein 14 | farnesoid x receptor

Type:

Nuclear Receptor

Mol. Mass.:

55916.24

Organism:

Homo sapiens (Human)

Description:

Q96RI1

Residue:

486

Sequence:

MVMQFQGLENPIQISPHCSCTPSGFFMEMMSMKPAKGVLTEQVAGPLGQNLEVEPYSQYS
NVQFPQVQPQISSSSYYSNLGFYPQQPEEWYSPGIYELRRMPAETLYQGETEVAEMPVTK
KPRMGASAGRIKGDELCVVCGDRASGYHYNALTCEGCKGFFRRSITKNAVYKCKNGGNCV
MDMYMRRKCQECRLRKCKEMGMLAECMYTGLLTEIQCKSKRLRKNVKQHADQTVNEDSEG
RDLRQVTSTTKSCREKTELTPDQQTLLHFIMDSYNKQRMPQEITNKILKEEFSAEENFLI
LTEMATNHVQVLVEFTKKLPGFQTLDHEDQIALLKGSAVEAMFLRSAEIFNKKLPSGHSD
LLEERIRNSGISDEYITPMFSFYKSIGELKMTQEEYALLTAIVILSPDRQYIKDREAVEK
LQEPLLDVLQKLCKIHQPENPQHFACLLGRLTELRTFNHHHAEMLMSWRVNDHKFTPLLC
EIWDVQ

BDBM30329

Biotinylated SRC-1 Peptide

Name:

Biotinylated SRC-1 Peptide

Synonyms:

n/a

Type:

Peptide

Mol. Mass.:

3599.04

Organism:

n/a

Description:

n/a

Residue:

Sequence:

biotin-CPSSHSSLTERHKILHRLLQEGSPS-CONH2