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Target
Poly [ADP-ribose] polymerase tankyrase-1
Ligand
BDBM75029
Substrate
n/a
Meas. Tech.
ChEMBL_1663210 (CHEMBL4012891)
IC50
251±n/a nM
Citation
 Thomson, DW; Wagner, AJ; Bantscheff, M; Benson, RE; Dittus, L; Duempelfeld, B; Drewes, G; Krause, J; Moore, JT; Mueller, K; Poeckel, D; Rau, C; Salzer, E; Shewchuk, L; Hopf, C; Emery, JG; Muelbaier, M Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines. J Med Chem 60:5455-5471 (2017) [PubMed]  Article 
Target
Name:
Poly [ADP-ribose] polymerase tankyrase-1
Synonyms:
(ARTD5 or PARP5a) | PARP5A | PARPL | Poly [ADP-ribose] polymerase 5 (PARP5) | Poly [ADP-ribose] polymerase tankyrase-1 | TIN1 | TINF1 | TNKS | TNKS1 | TNKS1_HUMAN | Tankyrase 1 | Tankyrase 1/2 | Tankyrase-1 | Tankyrase-1 (TNKS-1) | Tankyrase-1 (TNKS1)
Type:
Enzyme
Mol. Mass.:
142058.03
Organism:
Homo sapiens (Human)
Description:
O95271
Residue:
1327
Sequence:
MAASRRSQHHHHHHQQQLQPAPGASAPPPPPPPPLSPGLAPGTTPASPTASGLAPFASPRHGLALPEGDGSRDPPDRPRSPDPVDGTSCCSTTSTICTVAAAPVVPAVSTSSAAGVAPNPAGSGSNNSPSSSSSPTSSSSSSPSSPGSSLAESPEAAGVSSTAPLGPGAAGPGTGVPAVSGALRELLEACRNGDVSRVKRLVDAANVNAKDMAGRKSSPLHFAAGFGRKDVVEHLLQMGANVHARDDGGLIPLHNACSFGHAEVVSLLLCQGADPNARDNWNYTPLHEAAIKGKIDVCIVLLQHGADPNIRNTDGKSALDLADPSAKAVLTGEYKKDELLEAARSGNEEKLMALLTPLNVNCHASDGRKSTPLHLAAGYNRVRIVQLLLQHGADVHAKDKGGLVPLHNACSYGHYEVTELLLKHGACVNAMDLWQFTPLHEAASKNRVEVCSLLLSHGADPTLVNCHGKSAVDMAPTPELRERLTYEFKGHSLLQAAREADLAKVKKTLALEIINFKQPQSHETALHCAVASLHPKRKQVTELLLRKGANVNEKNKDFMTPLHVAAERAHNDVMEVLHKHGAKMNALDTLGQTALHRAALAGHLQTCRLLLSYGSDPSIISLQGFTAAQMGNEAVQQILSESTPIRTSDVDYRLLEASKAGDLETVKQLCSSQNVNCRDLEGRHSTPLHFAAGYNRVSVVEYLLHHGADVHAKDKGGLVPLHNACSYGHYEVAELLVRHGASVNVADLWKFTPLHEAAAKGKYEICKLLLKHGADPTKKNRDGNTPLDLVKEGDTDIQDLLRGDAALLDAAKKGCLARVQKLCTPENINCRDTQGRNSTPLHLAAGYNNLEVAEYLLEHGADVNAQDKGGLIPLHNAASYGHVDIAALLIKYNTCVNATDKWAFTPLHEAAQKGRTQLCALLLAHGADPTMKNQEGQTPLDLATADDIRALLIDAMPPEALPTCFKPQATVVSASLISPASTPSCLSAASSIDNLTGPLAELAVGGASNAGDGAAGTERKEGEVAGLDMNISQFLKSLGLEHLRDIFETEQITLDVLADMGHEELKEIGINAYGHRHKLIKGVERLLGGQQGTNPYLTFHCVNQGTILLDLAPEDKEYQSVEEEMQSTIREHRDGGNAGGIFNRYNVIRIQKVVNKKLRERFCHRQKEVSEENHNHHNERMLFHGSPFINAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTGCPTHKDRSCYICHRQMLFCRVTLGKSFLQFSTMKMAHAPPGHHSVIGRPSVNGLAYAEYVIYRGEQAYPEYLITYQIMKPEAPSQTATAAEQKT
  
Inhibitor
Name:
BDBM75029
Synonyms:
MLS000686692 | N-phenyl-4-tetrazolo[1,5-a]quinoxalinamine | N-phenyl-[1,2,3,4]tetrazolo[1,5-a]quinoxalin-4-amine | N-phenyltetrazolo[1,5-a]quinoxalin-4-amine | SMR000339750 | cid_1511413 | phenyl(tetrazolo[1,5-a]quinoxalin-4-yl)amine
Type:
Small organic molecule
Emp. Form.:
C14H10N6
Mol. Mass.:
262.2694
SMILES:
N(c1ccccc1)c1nc2ccccc2n2nnnc12
Structure:
Search PDB for entries with ligand similarity: