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Assay Detail

CHEMBL918244

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Binding
Inhibition of Rho kinase
ChEMBL ↗
52
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Rho-associated protein kinase (CHEMBL2111459) ↗
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design and synthesis of Rho kinase inhibitors (II).
Iwakubo M, Takami A, Okada Y, Kawata T, Tagami Y, Ohashi H, Sato M, Sugiyama T, Fukushima K, Iijima H.
Bioorg Med Chem (2007) 15 : 350 -364
PubMed 17046269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.21 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224594 — — 1 8.52
CHEMBL225166 — — 1 8.52
CHEMBL373512 — — 1 8.30
CHEMBL388516 — — 1 8.05
CHEMBL224510 — — 1 8.00
CHEMBL225582 — — 1 8.00
CHEMBL224535 — — 1 8.00
CHEMBL426925 — — 1 7.96
CHEMBL224166 — — 1 7.96
CHEMBL390837 — — 1 7.89
CHEMBL225637 — — 1 7.80
CHEMBL415061 — — 1 7.75
CHEMBL389168 — — 1 7.72
CHEMBL225224 — — 1 7.70
CHEMBL224885 — — 2 7.70
CHEMBL390389 — — 1 7.70
CHEMBL427245 — — 1 7.62
CHEMBL224509 — — 1 7.60
CHEMBL386937 — — 1 7.50
CHEMBL390736 — — 1 7.46
CHEMBL388742 — — 1 7.35
CHEMBL225167 — — 1 7.19
CHEMBL224746 — — 1 7.14
CHEMBL389622 — — 1 7.10
CHEMBL427254 — — 1 7.07
CHEMBL225560 — — 1 7.07
CHEMBL389915 — — 1 7.06
CHEMBL225434 — — 1 7.00
CHEMBL427083 — — 1 6.87
CHEMBL373487 — — 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224594 — IC50 = 3.0 nM 8.52
CHEMBL225166 — IC50 = 3.0 nM 8.52
CHEMBL373512 — IC50 = 5.0 nM 8.30
CHEMBL388516 — IC50 = 9.0 nM 8.05
CHEMBL225582 — IC50 = 10.0 nM 8.00
CHEMBL224535 — IC50 = 10.0 nM 8.00
CHEMBL224510 — IC50 = 10.0 nM 8.00
CHEMBL224166 — IC50 = 11.0 nM 7.96
CHEMBL426925 — IC50 = 11.0 nM 7.96
CHEMBL390837 — IC50 = 13.0 nM 7.89
CHEMBL225637 — IC50 = 16.0 nM 7.80
CHEMBL415061 — IC50 = 18.0 nM 7.75
CHEMBL389168 — IC50 = 19.0 nM 7.72
CHEMBL224885 — IC50 = 20.0 nM 7.70
CHEMBL224885 — IC50 = 20.0 nM 7.70
CHEMBL390389 — IC50 = 20.0 nM 7.70
CHEMBL225224 — IC50 = 20.0 nM 7.70
CHEMBL427245 — IC50 = 24.0 nM 7.62
CHEMBL224509 — IC50 = 25.0 nM 7.60
CHEMBL386937 — IC50 = 32.0 nM 7.50
CHEMBL390736 — IC50 = 35.0 nM 7.46
CHEMBL388742 — IC50 = 45.0 nM 7.35
CHEMBL225167 — IC50 = 65.0 nM 7.19
CHEMBL224746 — IC50 = 72.0 nM 7.14
CHEMBL389622 — IC50 = 80.0 nM 7.10
CHEMBL427254 — IC50 = 85.0 nM 7.07
CHEMBL225560 — IC50 = 85.0 nM 7.07
CHEMBL389915 — IC50 = 87.0 nM 7.06
CHEMBL225434 — IC50 = 100.0 nM 7.00
CHEMBL427083 — IC50 = 136.0 nM 6.87
CHEMBL373487 — IC50 = 150.0 nM 6.82
CHEMBL541388 FASUDIL HYDROCHLORIDE IC50 = 180.0 nM 6.75
CHEMBL225168 — IC50 = 180.0 nM 6.75
CHEMBL224533 — IC50 = 190.0 nM 6.72
CHEMBL224887 — IC50 = 220.0 nM 6.66
CHEMBL224500 — IC50 = 240.0 nM 6.62
CHEMBL224696 — IC50 = 240.0 nM 6.62
CHEMBL225282 — IC50 = 260.0 nM 6.58
CHEMBL224559 — IC50 = 290.0 nM 6.54
CHEMBL225225 — IC50 = 290.0 nM 6.54
CHEMBL390390 — IC50 = 320.0 nM 6.50
CHEMBL427085 — IC50 = 340.0 nM 6.47
CHEMBL224558 — IC50 = 440.0 nM 6.36
CHEMBL224067 — IC50 = 520.0 nM 6.28
CHEMBL223651 — IC50 = 540.0 nM 6.27
CHEMBL223553 — IC50 = 780.0 nM 6.11
CHEMBL224076 — IC50 = 7900.0 nM 5.10
CHEMBL224119 — IC50 > 10000.0 nM -
CHEMBL225226 — IC50 > 10000.0 nM -
CHEMBL224167 — IC50 > 1000.0 nM -