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Assay Detail

CHEMBL762182

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Binding
Inhibition constant against peptidyl prolyl isomerase
ChEMBL ↗
64
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Structure-activity studies of synthetic FKBP ligands as peptidyl-prolyl isomerase inhibitors
Holt DA, Konialian-Beck AL, Oh H, Yen H, Rozamus LW, Krog AJ, Erhard KF, Ortiz E, Levy MA, Brandt M, Bossard MJ, Luengo JI
Bioorg Med Chem Lett (1994) 4 : 315 -320
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 64 6.39 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110207 — — 1 8.15
CHEMBL108664 — — 1 8.05
CHEMBL108236 — — 1 8.05
CHEMBL321637 — — 1 8.00
CHEMBL110992 — — 1 8.00
CHEMBL299152 — — 1 7.92
CHEMBL111776 — — 1 7.70
CHEMBL108943 — — 3 7.70
CHEMBL107972 — — 1 7.64
CHEMBL300040 — — 1 7.57
CHEMBL109134 — — 1 7.46
CHEMBL111349 — — 1 7.26
CHEMBL326681 — — 1 7.22
CHEMBL108342 — — 1 7.22
CHEMBL322087 — — 1 7.16
CHEMBL420484 — — 1 7.02
CHEMBL108755 — — 1 7.00
CHEMBL49964 — — 1 6.96
CHEMBL326257 — — 1 6.80
CHEMBL108247 — — 1 6.78
CHEMBL107698 — — 1 6.73
CHEMBL326426 — — 1 6.70
CHEMBL324400 — — 1 6.70
CHEMBL109093 — — 1 6.70
CHEMBL109278 — — 1 6.64
CHEMBL108450 — — 1 6.60
CHEMBL108665 — — 1 6.60
CHEMBL105865 — — 1 6.52
CHEMBL321038 — — 1 6.52
CHEMBL108718 — — 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110207 — Ki = 7.0 nM 8.15
CHEMBL108664 — Ki = 9.0 nM 8.05
CHEMBL108236 — Ki = 9.0 nM 8.05
CHEMBL110992 — Ki = 10.0 nM 8.00
CHEMBL321637 — Ki = 10.0 nM 8.00
CHEMBL299152 — Ki = 12.0 nM 7.92
CHEMBL111776 — Ki = 20.0 nM 7.70
CHEMBL108943 — Ki = 20.0 nM 7.70
CHEMBL107972 — Ki = 23.0 nM 7.64
CHEMBL300040 — Ki = 27.0 nM 7.57
CHEMBL109134 — Ki = 35.0 nM 7.46
CHEMBL111349 — Ki = 55.0 nM 7.26
CHEMBL326681 — Ki = 60.0 nM 7.22
CHEMBL108342 — Ki = 60.0 nM 7.22
CHEMBL322087 — Ki = 70.0 nM 7.16
CHEMBL420484 — Ki = 95.0 nM 7.02
CHEMBL108755 — Ki = 100.0 nM 7.00
CHEMBL49964 — Ki = 110.0 nM 6.96
CHEMBL326257 — Ki = 160.0 nM 6.80
CHEMBL108247 — Ki = 165.0 nM 6.78
CHEMBL107698 — Ki = 186.0 nM 6.73
CHEMBL326426 — Ki = 200.0 nM 6.70
CHEMBL108943 — Ki = 200.0 nM 6.70
CHEMBL324400 — Ki = 200.0 nM 6.70
CHEMBL109093 — Ki = 200.0 nM 6.70
CHEMBL109278 — Ki = 230.0 nM 6.64
CHEMBL108943 — Ki = 250.0 nM 6.60
CHEMBL108450 — Ki = 250.0 nM 6.60
CHEMBL108665 — Ki = 250.0 nM 6.60
CHEMBL321038 — Ki = 300.0 nM 6.52
CHEMBL105865 — Ki = 300.0 nM 6.52
CHEMBL108718 — Ki = 330.0 nM 6.48
CHEMBL107759 — Ki = 340.0 nM 6.47
CHEMBL108390 — Ki = 400.0 nM 6.40
CHEMBL108985 — Ki = 410.0 nM 6.39
CHEMBL51641 — Ki = 660.0 nM 6.18
CHEMBL323035 — Ki = 1000.0 nM 6.00
CHEMBL107866 — Ki = 1000.0 nM 6.00
CHEMBL111587 — Ki = 1000.0 nM 6.00
CHEMBL413 SIROLIMUS Ki = 1000.0 nM 6.00
CHEMBL108192 — Ki = 1600.0 nM 5.80
CHEMBL324679 — Ki = 2000.0 nM 5.70
CHEMBL321392 — Ki = 2000.0 nM 5.70
CHEMBL108132 — Ki = 2000.0 nM 5.70
CHEMBL109633 — Ki = 2300.0 nM 5.64
CHEMBL324866 — Ki = 4000.0 nM 5.40
CHEMBL108662 — Ki = 4300.0 nM 5.37
CHEMBL320041 — Ki = 6000.0 nM 5.22
CHEMBL106706 — Ki = 8000.0 nM 5.10
CHEMBL109298 — Ki = 8000.0 nM 5.10