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Assay Detail

CHEMBL4402140

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

Binding
Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing measured for 5 to 10 secs by phenol red-based stopped-flow CO2 hydration assay
22
Total Activities
22
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 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors.
Lolak N, Akocak S, Bua S, Sanku RKK, Supuran CT.
Bioorg Med Chem (2019) 27 : 1588 -1594
PubMed 30846402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.07 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4568027 1 6.91
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.60
CHEMBL4448979 1 6.42
CHEMBL4552193 1 6.38
CHEMBL4587801 1 6.36
CHEMBL4574353 1 6.34
CHEMBL4539483 1 6.28
CHEMBL4452439 1 6.23
CHEMBL4552490 1 6.17
CHEMBL4444999 1 6.14
CHEMBL4451848 1 6.14
CHEMBL4462536 1 6.13
CHEMBL4456216 1 6.08
CHEMBL4557185 1 6.08
CHEMBL4461238 1 6.06
CHEMBL4467853 1 6.03
CHEMBL4537582 1 5.91
CHEMBL4458581 1 5.88
CHEMBL4556985 1 5.49
CHEMBL1615281 SLC-0111 1.0 1 5.29
CHEMBL4447240 1 5.28
CHEMBL4547531 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4568027 Ki = 122.1 nM 6.91
CHEMBL20 ACETAZOLAMIDE Ki = 250.0 nM 6.60
CHEMBL4448979 Ki = 381.6 nM 6.42
CHEMBL4552193 Ki = 415.4 nM 6.38
CHEMBL4587801 Ki = 441.7 nM 6.36
CHEMBL4574353 Ki = 458.7 nM 6.34
CHEMBL4539483 Ki = 522.2 nM 6.28
CHEMBL4452439 Ki = 591.3 nM 6.23
CHEMBL4552490 Ki = 681.1 nM 6.17
CHEMBL4444999 Ki = 722.9 nM 6.14
CHEMBL4451848 Ki = 724.3 nM 6.14
CHEMBL4462536 Ki = 736.8 nM 6.13
CHEMBL4456216 Ki = 829.6 nM 6.08
CHEMBL4557185 Ki = 840.9 nM 6.08
CHEMBL4461238 Ki = 864.2 nM 6.06
CHEMBL4467853 Ki = 935.8 nM 6.03
CHEMBL4537582 Ki = 1225.3 nM 5.91
CHEMBL4458581 Ki = 1317.4 nM 5.88
CHEMBL4556985 Ki = 3265.4 nM 5.49
CHEMBL1615281 SLC-0111 Ki = 5080.0 nM 5.29
CHEMBL4447240 Ki = 5312.5 nM 5.28
CHEMBL4547531 Ki = 5886.8 nM 5.23