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Target
Peregrin
Ligand
BDBM50148549
Substrate
n/a
Meas. Tech.
Alpha Screen competitive assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
270±180 nM
Comments
extracted
Citation
 Meier, JC; Tallant, C; Fedorov, O; Witwicka, H; Hwang, SY; van Stiphout, RG; Lambert, JP; Rogers, C; Yapp, C; Gerstenberger, BS; Fedele, V; Savitsky, P; Heidenreich, D; Daniels, DL; Owen, DR; Fish, PV; Igoe, NM; Bayle, ED; Haendler, B; Oppermann, UCT; Buffa, F; Brennan, PE; Müller, S; Gingras, AC; Odgren, PR; Birnbaum, MJ; Knapp, S Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol 12:2619-2630 (2017) [PubMed]  Article 
Target
Name:
Peregrin
Synonyms:
BR140 | BRPF1 | BRPF1_HUMAN | Bromodomain and PHD finger-containing protein 1 | Peregrin | Protein Br140
Type:
PROTEIN
Mol. Mass.:
137524.47
Organism:
Human
Description:
ChEMBL_108054
Residue:
1214
Sequence:
MGVDFDVKTFCHNLRATKPPYECPVETCRKVYKSYSGIEYHLYHYDHDNPPPPQQTPLRKHKKKGRQSRPANKQSPSPSEVSQSPGREVMSYAQAQRMVEVDLHGRVHRISIFDNLDVVSEDEEAPEEAPENGSNKENTETPAATPKSGKHKNKEKRKDSNHHHHHNVSASTTPKLPEVVYRELEQDTPDAPPRPTSYYRYIEKSAEELDEEVEYDMDEEDYIWLDIMNERRKTEGVSPIPQEIFEYLMDRLEKESYFESHNKGDPNALVDEDAVCCICNDGECQNSNVILFCDMCNLAVHQECYGVPYIPEGQWLCRRCLQSPSRAVDCALCPNKGGAFKQTDDGRWAHVVCALWIPEVCFANTVFLEPIDSIEHIPPARWKLTCYICKQRGSGACIQCHKANCYTAFHVTCAQQAGLYMKMEPVRETGANGTSFSVRKTAYCDIHTPPGSARRLPALSHSEGEEDEDEEEDEGKGWSSEKVKKAKAKSRIKMKKARKILAEKRAAAPVVSVPCIPPHRLSKITNRLTIQRKSQFMQRLHSYWTLKRQSRNGVPLLRRLQTHLQSQRNCDQVGRDSEDKNWALKEQLKSWQRLRHDLERARLLVELIRKREKLKRETIKVQQIAMEMQLTPFLILLRKTLEQLQEKDTGNIFSEPVPLSEVPDYLDHIKKPMDFFTMKQNLEAYRYLNFDDFEEDFNLIVSNCLKYNAKDTIFYRAAVRLREQGGAVLRQARRQAEKMGIDFETGMHIPHSLAGDEATHHTEDAAEEERLVLLENQKHLPVEEQLKLLLERLDEVNASKQSVGRSRRAKMIKKEMTALRRKLAHQRETGRDGPERHGPSSRGSLTPHPAACDKDGQTDSAAEESSSQETSKGLGPNMSSTPAHEVGRRTSVLFSKKNPKTAGPPKRPGRPPKNRESQMTPSHGGSPVGPPQLPIMSSLRQRKRGRSPRPSSSSDSDSDKSTEDPPMDLPANGFSGGNQPVKKSFLVYRNDCSLPRSSSDSESSSSSSSSAASDRTSTTPSKQGRGKPSFSRGTFPEDSSEDTSGTENEAYSVGTGRGVGHSMVRKSLGRGAGWLSEDEDSPLDALDLVWAKCRGYPSYPALIIDPKMPREGMFHHGVPIPVPPLEVLKLGEQMTQEAREHLYLVLFFDNKRTWQWLPRTKLVPLGVNQDLDKEKMLEGRKSNIRKSVQIAYHRALQHRSKVQGEQSSETSDSD
  
Inhibitor
Name:
BDBM50148549
Synonyms:
4-Bromo-N-(2,3-dihydro-6-methoxy-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl)-2-methyl-benzenesulfonamide | 4-Bromo-N-(2,3-dihydro-6-methoxy-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl)-2-methylbenzenesulfonamide | CHEMBL3770173 | OF 1 | OF-1
Type:
Small organic molecule
Emp. Form.:
C17H18BrN3O4S
Mol. Mass.:
440.312
SMILES:
COc1cc2n(C)c(=O)n(C)c2cc1NS(=O)(=O)c1ccc(Br)cc1C
Structure:
Search PDB for entries with ligand similarity: