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Assay Detail

CHEMBL1066299

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Functional
Antineuroinflammatory activity in LPS-stimulated rat neonatal microglia assessed as inhibition of PMA-induced superoxide anion production preincubated 15 mins prior to PMA challenge measured after 70 mins
20
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Microglia
Confidence 1 — Organism
Curated By Autocuration

Publication

Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections.
Peng J, Kudrimoti S, Prasanna S, Odde S, Doerksen RJ, Pennaka HK, Choo YM, Rao KV, Tekwani BL, Madgula V, Khan SI, Wang B, Mayer AM, Jacob MR, Tu LC, Gertsch J, Hamann MT.
J Med Chem (2010) 53 : 61 -76
PubMed 20017491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.10 7.52
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL579148 1 7.52
CHEMBL578331 9-N-NEOPENTYLMANZAMINE A 1 7.16
CHEMBL403233 MANZAMINE A 1 7.00
CHEMBL578532 6-METHOXYMANZAMINE A 1 7.00
CHEMBL592429 9-N-BUTYLMANZAMINE A 1 6.92
CHEMBL578914 1 5.66
CHEMBL592631 MANZAMINE D 1 5.61
CHEMBL592610 9-N-PROPYLMANZAMINE A 1 5.52
CHEMBL578725 9-N-ISOPENTYLMANZAMINE A 1 5.50
CHEMBL578116 9-N-ISOBUTYLMANZAMINE A 1 5.24
CHEMBL579152 1 5.07
CHEMBL592629 9-N-ETHYLMANZAMINE A 1 5.01
CHEMBL332054 IRCINAL 1 -
CHEMBL578745 1 -
CHEMBL437596 TETRAHYDROMANZAMINE A 2 -
CHEMBL592237 9-N-METHYLMANZAMINE A 1 -
CHEMBL612054 1 -
CHEMBL443503 15,16,32,33-TETRAHYDRO-8-HYDROXYMANZAMINE A 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL579148 IC50 = 30.0 nM 7.52
CHEMBL578331 9-N-NEOPENTYLMANZAMINE A IC50 = 70.0 nM 7.16
CHEMBL403233 MANZAMINE A IC50 = 100.0 nM 7.00
CHEMBL578532 6-METHOXYMANZAMINE A IC50 = 100.0 nM 7.00
CHEMBL592429 9-N-BUTYLMANZAMINE A IC50 = 120.0 nM 6.92
CHEMBL578914 IC50 = 2200.0 nM 5.66
CHEMBL592631 MANZAMINE D IC50 = 2450.0 nM 5.61
CHEMBL592610 9-N-PROPYLMANZAMINE A IC50 = 3000.0 nM 5.52
CHEMBL578725 9-N-ISOPENTYLMANZAMINE A IC50 = 3200.0 nM 5.50
CHEMBL578116 9-N-ISOBUTYLMANZAMINE A IC50 = 5700.0 nM 5.24
CHEMBL579152 IC50 = 8600.0 nM 5.07
CHEMBL592629 9-N-ETHYLMANZAMINE A IC50 = 9700.0 nM 5.01
CHEMBL437596 TETRAHYDROMANZAMINE A IC50 > 10000.0 nM -
CHEMBL612054 IC50 > 10000.0 nM -
CHEMBL592237 9-N-METHYLMANZAMINE A IC50 > 10000.0 nM -
CHEMBL443503 15,16,32,33-TETRAHYDRO-8-HYDROXYMANZAMINE A Activity - -
CHEMBL443503 15,16,32,33-TETRAHYDRO-8-HYDROXYMANZAMINE A IC50 > 10000.0 nM -
CHEMBL578745 IC50 > 10000.0 nM -
CHEMBL332054 IRCINAL IC50 > 10000.0 nM -
CHEMBL437596 TETRAHYDROMANZAMINE A Activity - -