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Target
Thyrotropin receptor
Ligand
BDBM60862
Substrate
n/a
Meas. Tech.
Antagonist Activity Assay
IC50
<100±n/a nM
Citation
 Karstens, WF; Conti, PG; Timmers, CM; Plate, R; Van Koppen, CJ TSH receptor antagonizing tetrahydroquinoline compounds US Patent  US9174940 Publication Date 11/3/2015
Target
Name:
Thyrotropin receptor
Synonyms:
LGR3 | TSH-R | TSHR | TSHR_HUMAN | Thyroid stimulating hormone receptor | Thyroid-stimulating hormone receptor | Thyroid-stimulating hormone receptor (TSH) | Thyrotropin receptor
Type:
Enzyme
Mol. Mass.:
86834.44
Organism:
Homo sapiens (Human)
Description:
P16473
Residue:
764
Sequence:
MRPADLLQLVLLLDLPRDLGGMGCSSPPCECHQEEDFRVTCKDIQRIPSLPPSTQTLKLIETHLRTIPSHAFSNLPNISRIYVSIDVTLQQLESHSFYNLSKVTHIEIRNTRNLTYIDPDALKELPLLKFLGIFNTGLKMFPDLTKVYSTDIFFILEITDNPYMTSIPVNAFQGLCNETLTLKLYNNGFTSVQGYAFNGTKLDAVYLNKNKYLTVIDKDAFGGVYSGPSLLDVSQTSVTALPSKGLEHLKELIARNTWTLKKLPLSLSFLHLTRADLSYPSHCCAFKNQKKIRGILESLMCNESSMQSLRQRKSVNALNSPLHQEYEENLGDSIVGYKEKSKFQDTHNNAHYYVFFEEQEDEIIGFGQELKNPQEETLQAFDSHYDYTICGDSEDMVCTPKSDEFNPCEDIMGYKFLRIVVWFVSLLALLGNVFVLLILLTSHYKLNVPRFLMCNLAFADFCMGMYLLLIASVDLYTHSEYYNHAIDWQTGPGCNTAGFFTVFASELSVYTLTVITLERWYAITFAMRLDRKIRLRHACAIMVGGWVCCFLLALLPLVGISSYAKVSICLPMDTETPLALAYIVFVLTLNIVAFVIVCCCYVKIYITVRNPQYNPGDKDTKIAKRMAVLIFTDFICMAPISFYALSAILNKPLITVSNSKILLVLFYPLNSCANPFLYAIFTKAFQRDVFILLSKFGICKRQAQAYRGQRVPPKNSTDIQVQKVTHDMRQGLHNMEDVYELIENSHLTPKKQGQISEEYMQTVL
  
Inhibitor
Name:
BDBM60862
Synonyms:
BDBM189328 | US9174940, 32
Type:
n/a
Emp. Form.:
C24H30N2O3
Mol. Mass.:
394.5066
SMILES:
CC(=O)N1CCC(C)(C2C=C(NC(=O)OC3CCCC3)C=CC12)c1ccccc1 |c:21,t:9|
Structure:
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