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Assay Detail

CHEMBL819364

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

Binding
Binding affinity against hERG Voltage-gated potassium channel subunit Kv11.1
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Publication

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Shu M, Loebach JL, Parker KA, Mills SG, Chapman KT, Shen DM, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Salvo JD, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.
Bioorg Med Chem Lett (2004) 14 : 947 -952
PubMed 15012999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.24 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL368329 1 6.40
CHEMBL367169 1 6.00
CHEMBL174214 1 5.68
CHEMBL172296 1 5.64
CHEMBL174004 1 5.52
CHEMBL176459 1 5.47
CHEMBL177033 1 5.46
CHEMBL176933 1 5.42
CHEMBL366328 1 5.25
CHEMBL176571 1 5.24
CHEMBL176426 1 5.22
CHEMBL366868 1 5.09
CHEMBL368204 1 5.02
CHEMBL172806 1 4.96
CHEMBL172854 1 4.85
CHEMBL367700 1 4.80
CHEMBL172090 1 4.66
CHEMBL174457 1 4.52
CHEMBL366871 1 4.43
CHEMBL367246 1 -
CHEMBL174304 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL368329 Ki = 400.0 nM 6.40
CHEMBL367169 Ki = 1000.0 nM 6.00
CHEMBL174214 Ki = 2100.0 nM 5.68
CHEMBL172296 Ki = 2300.0 nM 5.64
CHEMBL174004 Ki = 3000.0 nM 5.52
CHEMBL176459 Ki = 3400.0 nM 5.47
CHEMBL177033 Ki = 3500.0 nM 5.46
CHEMBL176933 Ki = 3800.0 nM 5.42
CHEMBL366328 Ki = 5600.0 nM 5.25
CHEMBL176571 Ki = 5700.0 nM 5.24
CHEMBL176426 Ki = 6000.0 nM 5.22
CHEMBL366868 Ki = 8100.0 nM 5.09
CHEMBL368204 Ki = 9600.0 nM 5.02
CHEMBL172806 Ki = 11000.0 nM 4.96
CHEMBL172854 Ki = 14000.0 nM 4.85
CHEMBL367700 Ki = 16000.0 nM 4.80
CHEMBL172090 Ki = 22000.0 nM 4.66
CHEMBL174457 Ki = 30000.0 nM 4.52
CHEMBL366871 Ki = 37000.0 nM 4.43
CHEMBL367246 Ki > 10000.0 nM -
CHEMBL174304 Ki > 10000.0 nM -