Reaction Details Report a problem with these data
Target
Thyrotropin receptor
Ligand
BDBM60844
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:
BDBM60844
Synonyms:
US9174940, 4
Type:
n/a
Emp. Form.:
C26H27N3O2
Mol. Mass.:
413.5115
SMILES:
CC(=O)N1c2ccc(NC(=O)c3ccccn3)cc2C(C)(CC1(C)C)c1ccccc1
Structure:
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