Target
Bromodomain-containing protein 1
Ligand
BDBM50032927
Substrate
n/a
Meas. Tech.
Alpha Screen competitive assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
3517±183 nM
Comments
extracted
Citation
 Meier, JCTallant, CFedorov, OWitwicka, HHwang, SYvan Stiphout, RGLambert, JPRogers, CYapp, CGerstenberger, BSFedele, VSavitsky, PHeidenreich, DDaniels, DLOwen, DRFish, PVIgoe, NMBayle, EDHaendler, BOppermann, UCTBuffa, FBrennan, PEMüller, SGingras, ACOdgren, PRBirnbaum, MJKnapp, 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:
Bromodomain-containing protein 1
Synonyms:
BR140-like protein | BRD1 | BRD1_HUMAN | BRL | BRL | BRPF2 | Bromodomain and PHD finger-containing protein 2 | Bromodomain-containing protein 1
Type:
PROTEIN
Mol. Mass.:
119557.65
Organism:
Homo sapiens (Human)
Description:
ChEMBL_105349
Residue:
1058
Sequence:
MRRKGRCHRGSAARHPSSPCSVKHSPTRETLTYAQAQRMVEIEIEGRLHRISIFDPLEIILEDDLTAQEMSECNSNKENSERPPVCLRTKRHKNNRVKKKNEALPSAHGTPASASALPEPKVRIVEYSPPSAPRRPPVYYKFIEKSAEELDNEVEYDMDEEDYAWLEIVNEKRKGDCVPAVSQSMFEFLMDRFEKESHCENQKQGEQQSLIDEDAVCCICMDGECQNSNVILFCDMCNLAVHQECYGVPYIPEGQWLCRHCLQSRARPADCVLCPNKGGAFKKTDDDRWGHVVCALWIPEVGFANTVFIEPIDGVRNIPPARWKLTCYLCKQKGVGACIQCHKANCYTAFHVTCAQKAGLYMKMEPVKELTGGGTTFSVRKTAYCDVHTPPGCTRRPLNIYGDVEMKNGVCRKESSVKTVRSTSKVRKKAKKAKKALAEPCAVLPTVCAPYIPPQRLNRIANQVAIQRKKQFVERAHSYWLLKRLSRNGAPLLRRLQSSLQSQRSSQQRENDEEMKAAKEKLKYWQRLRHDLERARLLIELLRKREKLKREQVKVEQVAMELRLTPLTVLLRSVLDQLQDKDPARIFAQPVSLKEVPDYLDHIKHPMDFATMRKRLEAQGYKNLHEFEEDFDLIIDNCMKYNARDTVFYRAAVRLRDQGGVVLRQARREVDSIGLEEASGMHLPERPAAAPRRPFSWEDVDRLLDPANRAHLGLEEQLRELLDMLDLTCAMKSSGSRSKRAKLLKKEIALLRNKLSQQHSQPLPTGPGLEGFEEDGAALGPEAGEEVLPRLETLLQPRKRSRSTCGDSEVEEESPGKRLDAGLTNGFGGARSEQEPGGGLGRKATPRRRCASESSISSSNSPLCDSSFNAPKCGRGKPALVRRHTLEDRSELISCIENGNYAKAARIAAEVGQSSMWISTDAAASVLEPLKVVWAKCSGYPSYPALIIDPKMPRVPGHHNGVTIPAPPLDVLKIGEHMQTKSDEKLFLVLFFDNKRSWQWLPKSKMVPLGIDETIDKLKMMEGRNSSIRKAVRIAFDRAMNHLSRVHGEPTSDLSDID
  
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:
Search PDB for entries with ligand similarity: