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TargetA disintegrin and metalloproteinase with thrombospondin motifs 1
LigandBDBM379557
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2125829 (CHEMBL4835174)
IC50>20000±n/a nM
Citation Brebion, FGosmini, RDeprez, PVarin, MPeixoto, CAlvey, LJary, HBienvenu, NTriballeau, NBlanque, RCottereaux, CChristophe, TVandervoort, NMollat, PTouitou, RLeonard, PDe Ceuninck, FBotez, IMonjardet, Avan der Aar, EAmantini, D Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis. J Med Chem64:2937-2952 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
A disintegrin and metalloproteinase with thrombospondin motifs 1
Name:A disintegrin and metalloproteinase with thrombospondin motifs 1
Synonyms:ADAMTS1 | ATS1_HUMAN | KIAA1346 | METH1
Type:PROTEIN
Mol. Mass.:105362.16
Organism:Homo sapiens (Human)
Description:ChEMBL_860059
Residue:967
Sequence:
MQRAVPEGFGRRKLGSDMGNAERAPGSRSFGPVPTLLLLAAALLAVSDALGRPSEEDEEL
VVPELERAPGHGTTRLRLHAFDQQLDLELRPDSSFLAPGFTLQNVGRKSGSETPLPETDL
AHCFYSGTVNGDPSSAAALSLCEGVRGAFYLLGEAYFIQPLPAASERLATAAPGEKPPAP
LQFHLLRRNRQGDVGGTCGVVDDEPRPTGKAETEDEDEGTEGEDEGAQWSPQDPALQGVG
QPTGTGSIRKKRFVSSHRYVETMLVADQSMAEFHGSGLKHYLLTLFSVAARLYKHPSIRN
SVSLVVVKILVIHDEQKGPEVTSNAALTLRNFCNWQKQHNPPSDRDAEHYDTAILFTRQD
LCGSQTCDTLGMADVGTVCDPSRSCSVIEDDGLQAAFTTAHELGHVFNMPHDDAKQCASL
NGVNQDSHMMASMLSNLDHSQPWSPCSAYMITSFLDNGHGECLMDKPQNPIQLPGDLPGT
SYDANRQCQFTFGEDSKHCPDAASTCSTLWCTGTSGGVLVCQTKHFPWADGTSCGEGKWC
INGKCVNKTDRKHFDTPFHGSWGMWGPWGDCSRTCGGGVQYTMRECDNPVPKNGGKYCEG
KRVRYRSCNLEDCPDNNGKTFREEQCEAHNEFSKASFGSGPAVEWIPKYAGVSPKDRCKL
ICQAKGIGYFFVLQPKVVDGTPCSPDSTSVCVQGQCVKAGCDRIIDSKKKFDKCGVCGGN
GSTCKKISGSVTSAKPGYHDIITIPTGATNIEVKQRNQRGSRNNGSFLAIKAADGTYILN
GDYTLSTLEQDIMYKGVVLRYSGSSAALERIRSFSPLKEPLTIQVLTVGNALRPKIKYTY
FVKKKKESFNAIPTFSAWVIEEWGECSKSCELGWQRRLVECRDINGQPASECAKEVKPAS
TRPCADHPCPQWQLGEWSSCSKTCGKGYKKRSLKCLSHDGGVLSHESCDPLKKPKHFIDF
CTMAECS
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  Blast E-value cutoff:
BDBM379557
n/a
NameBDBM379557
Synonyms:US9926281, Compound 36
TypeSmall organic molecule
Emp. Form.C20H25ClN4O3
Mol. Mass.404.891
SMILESCc1ccc(Cl)cc1N1CCN(CC1)C(=O)CCC1(NC(=O)NC1=O)C1CC1
Structure
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