Reaction Details |
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Target | Rho-associated protein kinase 2 |
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Ligand | BDBM50434485 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_961508 (CHEMBL2388366) |
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IC50 | >20000±n/a nM |
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Citation | Xiao, D; Palani, A; Huang, X; Sofolarides, M; Zhou, W; Chen, X; Aslanian, R; Guo, Z; Fossetta, J; Tian, F; Trivedi, P; Spacciapoli, P; Whitehurst, CE; Lundell, D Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors. Bioorg Med Chem Lett23:3262-6 (2013) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Rho-associated protein kinase 2 |
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Name: | Rho-associated protein kinase 2 |
Synonyms: | KIAA0619 | ROCK-II | ROCK2 | ROCK2_HUMAN | Rho kinase 2 (ROCKII) | Rho-associated protein kinase 2 (ROCK-2) | Rho-associated protein kinase 2 (ROCK2) | Rho-associated protein kinase 2 (ROCKII) | Rho-associated protein kinase 2/Transforming protein RhoA | Rho-associated, coiled-coil-containing protein kinase 2 | Rho-associated, coiled-coil-containing protein kinase II | Serine/threonine-protein kinase RIO2 | p164 ROCK-2 |
Type: | Protein |
Mol. Mass.: | 160885.43 |
Organism: | Homo sapiens (Human) |
Description: | O75116 |
Residue: | 1388 |
Sequence: | MSRPPPTGKMPGAPETAPGDGAGASRQRKLEALIRDPRSPINVESLLDGLNSLVLDLDFP
ALRKNKNIDNFLNRYEKIVKKIRGLQMKAEDYDVVKVIGRGAFGEVQLVRHKASQKVYAM
KLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNL
MSNYDVPEKWAKFYTAEVVLALDAIHSMGLIHRDVKPDNMLLDKHGHLKLADFGTCMKMD
ETGMVHCDTAVGTPDYISPEVLKSQGGDGFYGRECDWWSVGVFLYEMLVGDTPFYADSLV
GTYSKIMDHKNSLCFPEDAEISKHAKNLICAFLTDREVRLGRNGVEEIRQHPFFKNDQWH
WDNIRETAAPVVPELSSDIDSSNFDDIEDDKGDVETFPIPKAFVGNQLPFIGFTYYRENL
LLSDSPSCRETDSIQSRKNEESQEIQKKLYTLEEHLSNEMQAKEELEQKCKSVNTRLEKT
AKELEEEITLRKSVESALRQLEREKALLQHKNAEYQRKADHEADKKRNLENDVNSLKDQL
EDLKKRNQNSQISTEKVNQLQRQLDETNALLRTESDTAARLRKTQAESSKQIQQLESNNR
DLQDKNCLLETAKLKLEKEFINLQSALESERRDRTHGSEIINDLQGRICGLEEDLKNGKI
LLAKVELEKRQLQERFTDLEKEKSNMEIDMTYQLKVIQQSLEQEEAEHKATKARLADKNK
IYESIEEAKSEAMKEMEKKLLEERTLKQKVENLLLEAEKRCSLLDCDLKQSQQKINELLK
QKDVLNEDVRNLTLKIEQETQKRCLTQNDLKMQTQQVNTLKMSEKQLKQENNHLMEMKMN
LEKQNAELRKERQDADGQMKELQDQLEAEQYFSTLYKTQVRELKEECEEKTKLGKELQQK
KQELQDERDSLAAQLEITLTKADSEQLARSIAEEQYSDLEKEKIMKELEIKEMMARHKQE
LTEKDATIASLEETNRTLTSDVANLANEKEELNNKLKDVQEQLSRLKDEEISAAAIKAQF
EKQLLTERTLKTQAVNKLAEIMNRKEPVKRGNDTDVRRKEKENRKLHMELKSEREKLTQQ
MIKYQKELNEMQAQIAEESQIRIELQMTLDSKDSDIEQLRSQLQALHIGLDSSSIGSGPG
DAEADDGFPESRLEGWLSLPVRNNTKKFGWVKKYVIVSSKKILFYDSEQDKEQSNPYMVL
DIDKLFHVRPVTQTDVYRADAKEIPRIFQILYANEGESKKEQEFPVEPVGEKSNYICHKG
HEFIPTLYHFPTNCEACMKPLWHMFKPPPALECRRCHIKCHKDHMDKKEEIIAPCKVYYD
ISTAKNLLLLANSTEEQQKWVSRLVKKIPKKPPAPDPFARSSPRTSMKIQQNQSIRRPSR
QLAPNKPS
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BDBM50434485 |
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n/a |
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Name | BDBM50434485 |
Synonyms: | CHEMBL2385543 |
Type | Small organic molecule |
Emp. Form. | C34H29ClN4O2 |
Mol. Mass. | 561.073 |
SMILES | Clc1ccc(cc1)-c1cc2Cc3cc(ccc3N(Cc3ccccc3-c3cccnc3)C(=O)c2o1)N1CCNCC1 |
Structure |
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