Reaction Details Report a problem with these data
Target
Thyroid hormone receptor beta
Ligand
BDBM50178975
Substrate
n/a
Meas. Tech.
ChEMBL_338350 (CHEMBL865335)
EC50
4.7±n/a nM
Citation
 Garcia Collazo, AM; Koehler, KF; Garg, N; Färnegårdh, M; Husman, B; Ye, L; Ljunggren, J; Mellström, K; Sandberg, J; Grynfarb, M; Ahola, H; Malm, J Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta. Bioorg Med Chem Lett 16:1240-4 (2006) [PubMed]  Article 
Target
Name:
Thyroid hormone receptor beta
Synonyms:
ERBA2 | NR1A2 | Nuclear receptor subfamily 1 group A member 2 | THB_HUMAN | THR1 | THRB | c-erbA-2 | c-erbA-beta
Type:
Receptor
Mol. Mass.:
52793.62
Organism:
Homo sapiens (Human)
Description:
Recombinant hThR was obtained from nuclear extracts from SF9 cells infected with baculovirus vectors encoding for ThRbeta 1.
Residue:
461
Sequence:
MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQTTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYRCITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVLDDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWKQKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCEDQIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSLSSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPKLLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED
  
Inhibitor
Name:
BDBM50178975
Synonyms:
4,6-dichloro-5-(4-hydroxy-3-isopropylphenoxy)-1H-indole-2-carboxylic acid | CHEMBL203777
Type:
Small organic molecule
Emp. Form.:
C18H15Cl2NO4
Mol. Mass.:
380.222
SMILES:
CC(C)c1cc(Oc2c(Cl)cc3[nH]c(cc3c2Cl)C(O)=O)ccc1O
Structure:
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