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Assay Detail

CHEMBL4688199

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Binding
Inhibition of Plasmodium falciparum FLN
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Falcilysin (CHEMBL4295876)
Type SINGLE PROTEIN
Organism Plasmodium falciparum (isolate 3D7)

Publication

Structure guided development of potent piperazine-derived hydroxamic acid inhibitors targeting falcilysin.
Kahlon G,Lira R,Masvlov N,Pompa E,Brar N,Eagon S,Anderson MO,Andaya A,Chance JP,Fejzic H,Keniston A,Huynh N,Celis N,Vidal B,Trieu N,Rodriguez P,Mallari JP
Bioorg Med Chem Lett (2021) 32 : 127683 -127683
PubMed 33227414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 5.61 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4799253 1 6.66
CHEMBL4743280 1 6.22
CHEMBL4782486 1 6.05
CHEMBL4799260 1 6.00
CHEMBL4797916 1 5.96
CHEMBL4794156 1 5.85
CHEMBL4749474 1 5.85
CHEMBL4785958 1 5.77
CHEMBL4741390 1 5.60
CHEMBL4753948 1 5.60
CHEMBL4763576 1 5.58
CHEMBL4225532 1 5.52
CHEMBL4759772 1 5.46
CHEMBL4787612 1 5.40
CHEMBL4797275 1 5.40
CHEMBL4749198 1 5.40
CHEMBL4747594 1 5.40
CHEMBL4746210 1 5.31
CHEMBL4786923 1 5.30
CHEMBL4744749 1 5.05
CHEMBL4748768 1 5.00
CHEMBL4760331 1 4.96
CHEMBL4793336 1 -
CHEMBL4743581 1 -
CHEMBL4783383 1 -
CHEMBL4779972 1 -
CHEMBL4795927 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4799253 Ki = 220.0 nM 6.66
CHEMBL4743280 Ki = 600.0 nM 6.22
CHEMBL4782486 Ki = 900.0 nM 6.05
CHEMBL4799260 Ki = 1000.0 nM 6.00
CHEMBL4797916 Ki = 1100.0 nM 5.96
CHEMBL4794156 Ki = 1400.0 nM 5.85
CHEMBL4749474 Ki = 1400.0 nM 5.85
CHEMBL4785958 Ki = 1700.0 nM 5.77
CHEMBL4741390 Ki = 2500.0 nM 5.60
CHEMBL4753948 Ki = 2500.0 nM 5.60
CHEMBL4763576 Ki = 2600.0 nM 5.58
CHEMBL4225532 Ki = 3000.0 nM 5.52
CHEMBL4759772 Ki = 3500.0 nM 5.46
CHEMBL4787612 Ki = 4000.0 nM 5.40
CHEMBL4797275 Ki = 4000.0 nM 5.40
CHEMBL4749198 Ki = 4000.0 nM 5.40
CHEMBL4747594 Ki = 4000.0 nM 5.40
CHEMBL4746210 Ki = 4900.0 nM 5.31
CHEMBL4786923 Ki = 5000.0 nM 5.30
CHEMBL4744749 Ki = 9000.0 nM 5.05
CHEMBL4748768 Ki = 10000.0 nM 5.00
CHEMBL4760331 Ki = 11000.0 nM 4.96
CHEMBL4793336 Ki > 25000.0 nM -
CHEMBL4743581 Ki > 25000.0 nM -
CHEMBL4783383 Ki > 25000.0 nM -
CHEMBL4779972 Ki > 25000.0 nM -
CHEMBL4795927 Ki > 25000.0 nM -