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Assay Detail

CHEMBL4256842

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

Binding
Inhibition of human CA2 assessed as enzyme inhibitor complex formation preincubated for 15 mins and measured for 10 to 100 secs by phenol red dye based stopped-flow CO2 hydrase assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4-Hydroxy-3-(3-(phenylureido)benzenesulfonamides as SLC-0111 Analogues for the Treatment of Hypoxic Tumors Overexpressing Carbonic Anhydrase IX.
Bozdag M, Carta F, Ceruso M, Ferraroni M, McDonald PC, Dedhar S, Supuran CT.
J Med Chem (2018) 61 : 6328 -6338
PubMed 29962205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.07 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL4286620 1 7.03
CHEMBL4285851 1 6.86
CHEMBL4278617 1 6.43
CHEMBL4292591 1 6.43
CHEMBL4294703 1 6.17
CHEMBL4283637 1 6.14
CHEMBL4294527 1 6.12
CHEMBL4291115 1 6.11
CHEMBL4282079 1 6.08
CHEMBL1615281 SLC-0111 1.0 1 6.02
CHEMBL4282828 1 6.02
CHEMBL4288405 1 6.00
CHEMBL4279796 1 5.96
CHEMBL4287685 1 5.90
CHEMBL4286489 1 5.86
CHEMBL4292967 1 5.78
CHEMBL4287699 1 5.68
CHEMBL4292271 1 5.63
CHEMBL4289589 1 5.48
CHEMBL4293437 1 5.47
CHEMBL4289262 1 5.36
CHEMBL4284307 1 5.14
CHEMBL4294946 1 -
CHEMBL4290328 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL4286620 Ki = 94.3 nM 7.03
CHEMBL4285851 Ki = 136.9 nM 6.86
CHEMBL4278617 Ki = 373.2 nM 6.43
CHEMBL4292591 Ki = 368.7 nM 6.43
CHEMBL4294703 Ki = 667.8 nM 6.17
CHEMBL4283637 Ki = 728.5 nM 6.14
CHEMBL4294527 Ki = 762.3 nM 6.12
CHEMBL4291115 Ki = 771.7 nM 6.11
CHEMBL4282079 Ki = 842.3 nM 6.08
CHEMBL1615281 SLC-0111 Ki = 960.0 nM 6.02
CHEMBL4282828 Ki = 951.3 nM 6.02
CHEMBL4288405 Ki = 997.6 nM 6.00
CHEMBL4279796 Ki = 1107.5 nM 5.96
CHEMBL4287685 Ki = 1253.5 nM 5.90
CHEMBL4286489 Ki = 1394.7 nM 5.86
CHEMBL4292967 Ki = 1647.7 nM 5.78
CHEMBL4287699 Ki = 2103.1 nM 5.68
CHEMBL4292271 Ki = 2343.9 nM 5.63
CHEMBL4289589 Ki = 3333.8 nM 5.48
CHEMBL4293437 Ki = 3406.2 nM 5.47
CHEMBL4289262 Ki = 4416.5 nM 5.36
CHEMBL4284307 Ki = 7290.5 nM 5.14
CHEMBL4294946 Ki > 10000.0 nM -
CHEMBL4290328 Ki > 10000.0 nM -