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Target
Peregrin
Ligand
BDBM50032927
Substrate
n/a
Meas. Tech.
Alpha Screen competitive assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
172±10.0 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:
Homo sapiens (Human)
Description:
ChEMBL_108054
Residue:
1214
Sequence:
MGVDFDVKTFCHNLRATKPPYECPVETCRKVYKSYSGIEYHLYHYDHDNPPPPQQTPLRKHKKKGRQSRPANKQSPSPSEVSQSPGREVMSYAQAQRMVEVDLHGRVHRISIFDNLDVVSEDEEAPEEAPENGSNKENTETPAATPKSGKHKNKEKRKDSNHHHHHNVSASTTPKLPEVVYRELEQDTPDAPPRPTSYYRYIEKSAEELDEEVEYDMDEEDYIWLDIMNERRKTEGVSPIPQEIFEYLMDRLEKESYFESHNKGDPNALVDEDAVCCICNDGECQNSNVILFCDMCNLAVHQECYGVPYIPEGQWLCRRCLQSPSRAVDCALCPNKGGAFKQTDDGRWAHVVCALWIPEVCFANTVFLEPIDSIEHIPPARWKLTCYICKQRGSGACIQCHKANCYTAFHVTCAQQAGLYMKMEPVRETGANGTSFSVRKTAYCDIHTPPGSARRLPALSHSEGEEDEDEEEDEGKGWSSEKVKKAKAKSRIKMKKARKILAEKRAAAPVVSVPCIPPHRLSKITNRLTIQRKSQFMQRLHSYWTLKRQSRNGVPLLRRLQTHLQSQRNCDQVGRDSEDKNWALKEQLKSWQRLRHDLERARLLVELIRKREKLKRETIKVQQIAMEMQLTPFLILLRKTLEQLQEKDTGNIFSEPVPLSEVPDYLDHIKKPMDFFTMKQNLEAYRYLNFDDFEEDFNLIVSNCLKYNAKDTIFYRAAVRLREQGGAVLRQARRQAEKMGIDFETGMHIPHSLAGDEATHHTEDAAEEERLVLLENQKHLPVEEQLKLLLERLDEVNASKQSVGRSRRAKMIKKEMTALRRKLAHQRETGRDGPERHGPSSRGSLTPHPAACDKDGQTDSAAEESSSQETSKGLGPNMSSTPAHEVGRRTSVLFSKKNPKTAGPPKRPGRPPKNRESQMTPSHGGSPVGPPQLPIMSSLRQRKRGRSPRPSSSSDSDSDKSTEDPPMDLPANGFSGGNQPVKKSFLVYRNDCSLPRSSSDSESSSSSSSSAASDRTSTTPSKQGRGKPSFSRGTFPEDSSEDTSGTENEAYSVGTGRGVGHSMVRKSLGRGAGWLSEDEDSPLDALDLVWAKCRGYPSYPALIIDPKMPREGMFHHGVPIPVPPLEVLKLGEQMTQEAREHLYLVLFFDNKRTWQWLPRTKLVPLGVNQDLDKEKMLEGRKSNIRKSVQIAYHRALQHRSKVQGEQSSETSDSD
  
Inhibitor
Name:
BDBM50032927
Synonyms:
CHEMBL3356143 | N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide | PFI 4 | PFI-4 | PFI4
Type:
Small organic molecule
Emp. Form.:
C21H24N4O3
Mol. Mass.:
380.4403
SMILES:
COc1ccccc1C(=O)Nc1cc2n(C)c(=O)n(C)c2cc1N1CCCC1
Structure:
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