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Assay Detail

CHEMBL864467

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory activity against dynamin1 GTPase expressed in sheep brain
133
Total Activities
133
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Ovis aries
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Dynamin-1 (CHEMBL4958)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule inhibitors of dynamin I GTPase activity: development of dimeric tyrphostins.
Hill T, Odell LR, Edwards JK, Graham ME, McGeachie AB, Rusak J, Quan A, Abagyan R, Scott JL, Robinson PJ, McCluskey A.
J Med Chem (2005) 48 : 7781 -7788
PubMed 16302817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 133 4.99 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67535 1 5.77
CHEMBL199469 1 5.77
CHEMBL196854 1 5.77
CHEMBL198466 1 5.77
CHEMBL358746 1 5.68
CHEMBL144589 1 5.50
CHEMBL197374 1 5.30
CHEMBL144842 1 5.30
CHEMBL144908 1 5.29
CHEMBL198705 1 5.29
CHEMBL197068 1 5.22
CHEMBL198573 1 5.10
CHEMBL197017 1 5.10
CHEMBL198915 1 5.05
CHEMBL144760 1 4.58
CHEMBL197388 1 4.42
CHEMBL445859 1 4.38
CHEMBL371526 1 4.21
CHEMBL77030 TYRPHOSTIN 47 1 4.16
CHEMBL371102 1 4.10
CHEMBL144159 1 4.08
CHEMBL371303 1 4.02
CHEMBL296407 1 -
CHEMBL197490 1 -
CHEMBL371282 1 -
CHEMBL197177 1 -
CHEMBL197015 1 -
CHEMBL198919 1 -
CHEMBL425207 1 -
CHEMBL197425 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67535 IC50 = 1700.0 nM 5.77
CHEMBL198466 IC50 = 1700.0 nM 5.77
CHEMBL196854 IC50 = 1700.0 nM 5.77
CHEMBL199469 IC50 = 1700.0 nM 5.77
CHEMBL358746 IC50 = 2100.0 nM 5.68
CHEMBL144589 IC50 = 3200.0 nM 5.50
CHEMBL197374 IC50 = 5000.0 nM 5.30
CHEMBL144842 IC50 = 5000.0 nM 5.30
CHEMBL144908 IC50 = 5100.0 nM 5.29
CHEMBL198705 IC50 = 5100.0 nM 5.29
CHEMBL197068 IC50 = 6000.0 nM 5.22
CHEMBL198573 IC50 = 8000.0 nM 5.10
CHEMBL197017 IC50 = 8000.0 nM 5.10
CHEMBL198915 IC50 = 9000.0 nM 5.05
CHEMBL144760 IC50 = 26000.0 nM 4.58
CHEMBL197388 IC50 = 38000.0 nM 4.42
CHEMBL445859 IC50 = 42000.0 nM 4.38
CHEMBL371526 IC50 = 61000.0 nM 4.21
CHEMBL77030 TYRPHOSTIN 47 IC50 = 70000.0 nM 4.16
CHEMBL371102 IC50 = 80000.0 nM 4.10
CHEMBL144159 IC50 = 84000.0 nM 4.08
CHEMBL371303 IC50 = 95000.0 nM 4.02
CHEMBL199265 IC50 > 100000.0 nM -
CHEMBL425390 IC50 > 100000.0 nM -
CHEMBL380566 IC50 > 100000.0 nM -
CHEMBL200345 IC50 > 100000.0 nM -
CHEMBL198885 IC50 >= 100000.0 nM -
CHEMBL198627 IC50 > 100000.0 nM -
CHEMBL427373 IC50 > 100000.0 nM -
CHEMBL198585 IC50 >= 100000.0 nM -
CHEMBL198838 IC50 >= 100000.0 nM -
CHEMBL198889 IC50 >= 100000.0 nM -
CHEMBL382758 IC50 >= 100000.0 nM -
CHEMBL371768 IC50 >= 100000.0 nM -
CHEMBL198626 IC50 > 100000.0 nM -
CHEMBL198901 IC50 > 100000.0 nM -
CHEMBL199009 IC50 >= 100000.0 nM -
CHEMBL381439 IC50 >= 100000.0 nM -
CHEMBL382303 IC50 >= 100000.0 nM -
CHEMBL198751 IC50 >= 100000.0 nM -
CHEMBL197486 IC50 >= 100000.0 nM -
CHEMBL199184 IC50 >= 100000.0 nM -
CHEMBL198484 IC50 >= 100000.0 nM -
CHEMBL199010 IC50 >= 100000.0 nM -
CHEMBL198528 IC50 >= 100000.0 nM -
CHEMBL372329 IC50 >= 100000.0 nM -
CHEMBL197238 IC50 >= 100000.0 nM -
CHEMBL198683 IC50 >= 100000.0 nM -
CHEMBL371093 IC50 >= 100000.0 nM -
CHEMBL370851 IC50 > 100000.0 nM -